https://proteopedia.org/api.php?action=feedcontributions&feedformat=atom&user=Wil+AndahazyProteopedia - User contributions [en]2026-09-26T21:01:09ZUser contributionsMediaWiki 1.43.8https://proteopedia.org/index.php?title=Belsomra&diff=2688878Belsomra2016-12-08T03:11:00Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' frame='' align='right' caption='' scene='74/746099/Belsomra/4' /><br />
<scene name='74/746099/Belsomra/4'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: http://dx.doi.org/10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are Gamma-aminobutyric acid (GABA) agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, Belsomra cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />. Due to the targeting of these receptors, a common side effect of Belsomra is somnolence, or next day drowsiness <ref>doi:10.5664/jcsm.6116</ref>.<br />
== Function ==<br />
The orexin neuropeptides, <scene name='74/746099/Orexin-a/1'>Orexin-A</scene> and <scene name='74/746099/Orexin-b/1'>Orexin-B</scene>, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref><ref>PMID:15479620</ref><ref>PMID:10583376</ref>. These orexin neuropeptides bind to two subtypes of receptors, [http://www.rcsb.org/pdb/explore/jmol.do?structureId=4ZJ8&residueNr=SUV Orexin receptor 1] and [http://www.rcsb.org/pdb/explore/jmol.do?structureId=4S0V&residueNr=SUV Orexin receptor 2], both of which are G protein coupled receptors (GPCRs) <ref>doi:10.1038/nsmb.3183</ref>. The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. When the neuropeptides bind to the receptors, an increase in calcium levels within the neurotransmitters lead the neurons to fire more frequently. Thus, binding of the two can control wakefulness in humans. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
Belsomra assumes a conformation similar to that of a horseshoe when binding to the [http://www.nature.com/nbt/journal/v32/n11/fig_tab/nbt.3028_F2.html orthosteric binding pocket] of either <scene name='74/746099/Orx1/3'>orexin receptor 1</scene> or <scene name='74/746099/Suvorexant/5'>orexin receptor 2</scene>. Through steric hindrance, this horseshoe conformation halts transmembrane domain movement by making contact with the alpha-helices of all transmembrane domains except for the first one upon entering the binding site of the receptor. <ref name="six"> doi: 10.1038/nature14035 </ref>. Types of interactions between Belsomra and both orexin receptor subtypes include Van Der Waals interactions, aromatic packing via the pi bonds of aromatic amino acids, and hydrogen bonding. The most significant hydrogen bond occurs between the amide of the orexin receptors’ <scene name='74/746099/Asn324_orx2/5'>Asn324</scene> and an amide on Belsomra. <ref name="six" />. Water molecules also play a role in hydrogen bonding via formation of bridges between the Belsomra drug itself and the orexin receptors’ Asn324 and <scene name='74/746099/His350/2'>His350</scene>. <ref name="six" />. Structural differences of the two orexin receptors’ binding sites involve only two amino acids: Thr135 in receptor 2 is Ala127 in receptor 1, while Thr111 in receptor 2 is Ser103 in receptor 1. <ref name="six" /><ref>doi:10.1038/nsmb.3198</ref>. <br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system<ref>Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125. doi: http://dx.doi.org/10.4088/PCC.v03n0303</ref>. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal<ref>doi:10.2174/157015908787386050</ref>. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder<ref>doi: 10.2147/DDDT.S73224</ref>.<br />
<br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688446Belsomra2016-12-05T20:30:24Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: http://dx.doi.org/10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are Gamma-aminobuyric acid (GABA) agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system<ref>Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125. doi: http://dx.doi.org/10.4088/PCC.v03n0303</ref>. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal<ref>doi:10.2174/157015908787386050</ref>. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder<ref>doi: 10.2147/DDDT.S73224</ref>.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688259Belsomra2016-12-04T21:57:24Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system<ref>Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.</ref>. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal<ref>doi:10.2174/157015908787386050</ref>. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder<ref>doi: 10.2147/DDDT.S73224</ref>.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688010Belsomra2016-11-29T01:07:52Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688009Belsomra2016-11-29T01:06:51Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<ref>doi:10.1002/prot.20251</ref><br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688004Belsomra2016-11-29T00:57:11Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688003Belsomra2016-11-29T00:56:10Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<ref>doi:10.1093/nar/gkp287</ref><br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688002Belsomra2016-11-28T19:40:24Z<p>Wil Andahazy: </p>
<hr />
<div><StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688001Belsomra2016-11-28T19:36:41Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption=scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2688000Belsomra2016-11-28T19:32:59Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687999Belsomra2016-11-28T18:59:09Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687998Belsomra2016-11-28T18:58:15Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<ref>doi:10.1093/database/bav120 </ref><br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687997Belsomra2016-11-28T18:57:30Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep (Sutton). Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687996Belsomra2016-11-28T18:57:11Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep (Sutton). Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687995Belsomra2016-11-28T18:54:15Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep (Sutton). Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687994Belsomra2016-11-28T18:42:20Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687993Belsomra2016-11-28T18:41:04Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>PMID:9491897 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687992Belsomra2016-11-28T18:40:05Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond <ref>doi:10.1016/S0092-8674(00)80949-6 </ref>. Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687991Belsomra2016-11-28T18:37:29Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors <ref name="two" />. Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur <ref name="one" />.<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687990Belsomra2016-11-28T18:34:41Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: 10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687989Belsomra2016-11-28T18:31:50Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">DOI:10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687988Belsomra2016-11-28T18:14:30Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref name="one">DOI:10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687987Belsomra2016-11-28T18:13:34Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref name="one">DOI: 10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />.<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687986Belsomra2016-11-28T18:11:33Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='4S0V' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>DOI: 10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1).<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687969Belsomra2016-11-28T00:18:34Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>DOI: 10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1).<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687968Belsomra2016-11-28T00:17:14Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>doi: 10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1).<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687967Belsomra2016-11-28T00:16:29Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>doi:10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1).<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687966Belsomra2016-11-28T00:15:21Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1).<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687965Belsomra2016-11-28T00:14:23Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1).<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687964Belsomra2016-11-28T00:12:07Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref>10.1097/01.NAJ.0000457406.61092.35</ref>. <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687963Belsomra2016-11-28T00:11:42Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687962Belsomra2016-11-28T00:11:05Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>10.1097/01.NAJ.0000457406.61092.35. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687961Belsomra2016-11-28T00:10:34Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>10.1097/01.NAJ.0000457406.61092.35<ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687960Belsomra2016-11-28T00:07:43Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687959Belsomra2016-11-27T23:56:57Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural Highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687958Belsomra2016-11-27T23:55:36Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687957Belsomra2016-11-27T23:54:40Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1).<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687956Belsomra2016-11-27T23:51:01Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687955Belsomra2016-11-27T23:48:19Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
<scene name='74/746099/Belsomra/1'>Belsomra</scene> is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687954Belsomra2016-11-27T23:48:16Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
3. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
4. Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
5. Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
6. Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
7. Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
8. T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding <br />
behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687953Belsomra2016-11-27T23:47:19Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
3. First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
4. Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
5. Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
6. Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
7. Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
8. T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. <br />
McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding <br />
behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687952Belsomra2016-11-27T23:46:01Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/><br />
<br />
First Orexin Receptor Antagonist Approved for Insomnia.<br />
AJN, American Journal of Nursing. 114(12):26, December 2014.<br />
<br />
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.<br />
<br />
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.<br />
<br />
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050<br />
<br />
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.<br />
<br />
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.</div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687951Belsomra2016-11-27T23:42:03Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687950Belsomra2016-11-27T23:39:33Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
== Function ==<br />
<br />
== Relevance ==<br />
<br />
== Structural highlights ==<br />
<br />
==Relationship to Insomnia==<br />
<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687949Belsomra2016-11-27T23:35:21Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
Background to Insomnia<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
== Function ==<br />
<br />
== Disease ==<br />
<br />
== Relevance ==<br />
<br />
== Structural highlights ==<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687948Belsomra2016-11-27T23:34:39Z<p>Wil Andahazy: </p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
== Background ==<br />
Abstract<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
Background to Insomnia<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
== Function ==<br />
<br />
== Disease ==<br />
<br />
== Relevance ==<br />
<br />
== Structural highlights ==<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazyhttps://proteopedia.org/index.php?title=Belsomra&diff=2687947Belsomra2016-11-27T23:27:32Z<p>Wil Andahazy: New page: ==Your Heading Here (maybe something like 'Structure')== 0 <StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''> This is a default text for y...</p>
<hr />
<div>==Your Heading Here (maybe something like 'Structure')== 0<br />
<StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''><br />
This is a default text for your page '''Belsomra'''. Click above on '''edit this page''' to modify. Be careful with the &lt; and &gt; signs.<br />
You may include any references to papers as in: the use of JSmol in Proteopedia <ref>DOI 10.1002/ijch.201300024</ref> or to the article describing Jmol <ref>PMID:21638687</ref> to the rescue.<br />
<br />
<br />
Abstract<br />
Belsomra is a medication used to treat the inability to fall asleep or stay asleep (1). While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin (2). Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep (1). <br />
<br />
<br />
Background to Insomnia<br />
Insomnia is a sleep disorder that is seen to be mostly caused by stress, and results in inefficient cooperation between the sleep and wake pathways of the arousal system. The branch of the arousal system that reaches the lateral hypothalamus, which contains the melanin-concentrated orexin neuropeptide signaling system, is one of the most significantly affected areas of the wakefulness network. This orexin system is a major promoter for wakefulness and is most active during efforts to sustain and maintain arousal, while showing little activity during sleep. Orexins show little activity during sleep because the systems to promote wakefulness are blocked by neurons of the ventrolateral preoptic nucleus and thus cannot fire. During sleep, these VLPO neurons are activated and form dense clusters containing GABA and galanin, which aid in their function as inhibitors for arousal. <br />
With insomnia, the structures regulating a patient’s arousal system are unusually active during sleep, and thus the system fails to deactivate. Belsomra is a drug that counteracts this by serving as a dual antagonist in its interactions with Orexin receptors 1 and 2, in the aim of deactivating the arousal system in order for patients to sleep with little orexin activity present. This could also exacerbate the symptoms of narcolepsy, as the already little orexin activity would be diminished at great risk to patients with the sleep disorder.<br />
<br />
== Function ==<br />
<br />
== Disease ==<br />
<br />
== Relevance ==<br />
<br />
== Structural highlights ==<br />
<br />
This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.<br />
<br />
</StructureSection><br />
== References ==<br />
<references/></div>Wil Andahazy