5-羟色胺（5-HT）受体的变构调节。
Allosteric modulation of the 5-HT(3) receptor.
机构信息
Department of Neuroscience, Tufts University, 136 Harrison Ave, Boston, MA 02111, USA.
出版信息
Curr Opin Pharmacol. 2011 Feb;11(1):75-80. doi: 10.1016/j.coph.2011.01.010. Epub 2011 Feb 20.
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.
摘要
5-羟色胺 3 型（5-HT（3））受体是配体门控离子通道，在抑郁、焦虑、药物滥用、呕吐、炎性疼痛、脊髓伤害感受、胃肠道功能和心血管反射中发挥重要作用。可能最受研究的 5-HT（3）受体调节剂是高亲和力竞争性“司琼”拮抗剂，以昂丹司琼为典型代表。然而，有广泛的化合物调节 5-HT（3）受体，不是通过正位点，而是通过结合变构位点。最值得注意的是某些靶标归属的治疗化合物，但在临床相关浓度下变构调节 5-HT（3）受体。
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