Belsomra: Difference between revisions

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<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" />.

<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" />.

== Function ==

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>. 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" />.

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 <StructureSection load='4S0V' size='340' frame='' align='right' caption='' scene='74/746099/Belsomra/4' />
-	<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" />.
+	<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" />.
 == Function ==
 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>. 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" />.