Department of Biochemistry, University of Cambridge, Cambridge CB2 1QW, UK.
J Biol Chem. 2012 Nov 23;287(48):40239-45. doi: 10.1074/jbc.R112.406496. Epub 2012 Oct 4.
5-Hydroxytryptamine type 3 (5-HT(3)) receptors are cation-selective Cys loop receptors found in both the central and peripheral nervous systems. There are five 5-HT(3) receptor subunits (A-E), and all functional receptors require at least one A subunit. Regions from noncontiguous parts of the subunit sequence contribute to the agonist-binding site, and the roles of a range of amino acid residues that form the binding pocket have been identified. Drugs that selectively antagonize 5-HT(3) receptors (the "setrons") are the current gold standard for treatment of chemotherapy-induced and postoperative nausea and vomiting and have potential for the treatment of a range of other conditions.
5-羟色胺 3 型（5-HT（3））受体是一种阳离子选择性半胱氨酸环受体，存在于中枢和外周神经系统中。有五种 5-HT（3）受体亚基（A-E），所有功能性受体至少需要一个 A 亚基。亚基序列不连续部分的区域有助于激动剂结合位点，并且已经确定了形成结合口袋的一系列氨基酸残基的作用。选择性拮抗 5-HT（3）受体的药物（“setrons”）是目前治疗化疗引起的和术后恶心和呕吐的金标准，并且有可能治疗一系列其他疾病。
