title: Allosteric modulation of the 5-HT(3) receptor.
abstract: 5-Hydroxytryptamine type 3 (5-HT(3)) receptors are ligand-gated ion channels that play important roles in depression, anxiety, substance abuse, emesis, inflammatory pain, spinal nociception, gastrointestinal function, and cardiovascular reflexes. Probably the most studied modulators of 5-HT(3) receptors are the high affinity competitive 'setron' antagonists typified by ondansetron. However, there exists a broad range of compounds that modulate the 5-HT(3) receptor, not through the orthosteric site but by binding to allosteric sites. Most notable are therapeutic compounds ascribed to certain targets but that allosterically modulate 5-HT(3) receptors at clinically relevant concentrations.
authors.affiliation: Department of Neuroscience, Tufts University, 136 Harrison Ave, Boston, MA 02111, USA. paul.davies@tufts.edu
authors.forename: Paul A
authors.initials: PA
authors.lastname: Davies
mesh_terms: D000495:Allosteric Site; D000818:Animals; D006801:Humans; D017294:Ondansetron / Q000494:pharmacology; D011485:Protein Binding; D044406:Receptors, Serotonin, 5-HT3 / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D044406:Receptors, Serotonin, 5-HT3; D017294:Ondansetron