Sandbox 77: Difference between revisions
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== General Function == | |||
<Structure load='4iar' size='300' frame='true' align='right' caption='Viewing Window' scene='Insert optional scene name here' /> | <Structure load='4iar' size='300' frame='true' align='right' caption='Viewing Window' scene='Insert optional scene name here' /> | ||
5-hydroxytryptamine (5-HT), Serotonin, receptors are found on the membrane of neurons in the central nervous system and peripheral nervous system. These receptors allow for the body to respond to serotonin and regulate many biological pathways. Serotonin, also known as 5 hydroxytryptamine, is an endogenous neurotransmitter made from tryptophan and is largely found in the gastrointestinal tract. It is known to regulate mood, appetite, digestion, circadian rhythm, learning and internal temperature regulation. It is can be an inhibitory or excitatory neurotransmitter that is released into the synaptic space and can bind to receptors on the postsynaptic neuron or be taken back up into the presynaptic neuron via Serotonin reuptake transporters.<ref>Goodsell D. ''Serotonin Receptor''. RCSB PDB-101 (2013) [http://www.rcsb.org/pdb/101/motm.do?momID=164 DOI: 10.2210/rcsb_pdb/mom_2013_8]</ref> 5-HT receptors are classified into 7 different subfamilies (5-HT1, 5-HT2, 5-HT3, etc.) by signaling mechanisms and homology of structure. All 5-HT receptors are known to have G-protein linked pathways except for the 5-HT3 receptor which acts as an ion channel. <ref name ="one">Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou EZ, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE. Structural Basis for Molecular Recognition at Serotonin Receptors. Science. 2013 May 3; 340(6132): 610–614. PMID:3644373 [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3644373/]</ref> | 5-hydroxytryptamine (5-HT), Serotonin, receptors are found on the membrane of neurons in the central nervous system and peripheral nervous system. These receptors allow for the body to respond to serotonin and regulate many biological pathways. Serotonin, also known as 5 hydroxytryptamine, is an endogenous neurotransmitter made from tryptophan and is largely found in the gastrointestinal tract. It is known to regulate mood, appetite, digestion, circadian rhythm, learning and internal temperature regulation. It is can be an inhibitory or excitatory neurotransmitter that is released into the synaptic space and can bind to receptors on the postsynaptic neuron or be taken back up into the presynaptic neuron via Serotonin reuptake transporters.<ref>Goodsell D. ''Serotonin Receptor''. RCSB PDB-101 (2013) [http://www.rcsb.org/pdb/101/motm.do?momID=164 DOI: 10.2210/rcsb_pdb/mom_2013_8]</ref> 5-HT receptors are classified into 7 different subfamilies (5-HT1, 5-HT2, 5-HT3, etc.) by signaling mechanisms and homology of structure. All 5-HT receptors are known to have G-protein linked pathways except for the 5-HT3 receptor which acts as an ion channel. <ref name ="one">Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou EZ, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE. Structural Basis for Molecular Recognition at Serotonin Receptors. Science. 2013 May 3; 340(6132): 610–614. PMID:3644373 [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3644373/]</ref> | ||
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== Structural highlights/Specific Function of 5-HT3== | == Structural highlights/Specific Function of 5-HT3== | ||
<scene name='71/716548/5-ht3_receptor/1'>The 5-HT3 receptor</scene> is a pentameric cation-selective ion channel and plays a role in neuronal excitation to release neurotransmitters from the postsynaptic neuron. Opening of the cation channel causes an influx of sodium and calcium through the receptor pore leading to a membrane depolarization. Five receptor subunits, A to E, have been found in humans but only subunits A and B have been found in rodents. When experimentally expressed in a host, the 5-HT3 receptor is comprised of either A or AB subunits which can result in a homopentameric receptor or a heteropentameric receptor respectively. The A and B subunits are found throughout the brain in areas such as the hippocampus and amygdala. 5-HT3 is a transmembrane channel that is stimulated to open state by the interaction of the receptor with serotonin in the extracellular space. The binding site is comprised of six loops from two adjacent subunits. Loops A, B and C form the principal subunit and loops D, E and F form the complementary subunit of the binding site in the extracellular N-terminal domain. Loop E contains tyrosine side chains which aid in the binding of serotonin.<ref>Hassaine G,Cedric D, Luigino G, Romain W, Menno BT, Ruud H, Alexandra G, Henning S, Takashi T, Aline D, Christophe M, Xiao-Dan L, Frederic P, Horst V, Hugues N. ''X-ray Structure of the Mouse Serotonin 5-HT3 Receptor. Nature 512.7514 (2014): 276-81.[http://www.nature.com/nature/journal/v512/n7514/full/nature13552.html DOI:10.1038/nature13552]</ref> The transmembrane region is comprised of multiple alpha helical structures and mediates ion flow and ion specificity<ref> Thompson AJ, Lummis SCR. 5-HT3 Receptors. Curr Pharm Des. 2006; 12(28): 3615–3630. PMID:2664614 [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2664614/]</ref> | |||
== 5-HT1B (and 5HT-2B) receptor agonists: Lysergic Acid Diethylamide (LSD)== | == 5-HT1B (and 5HT-2B) receptor agonists: Lysergic Acid Diethylamide (LSD)== | ||
