5-HT4 receptors: History, molecular pharmacology and brain functions
5-HT4 receptors: History, molecular pharmacology and brain functions
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DOI：
10.1016/j.neuropharm.2008.05.013
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发表时间：
2008-11-01
影响因子：
4.7
通讯作者：
Dumuis, Aline
中科院分区：
文献类型：
--
作者：
Bockaert, Joel;Claeysen, Sylvie;Dumuis, Aline
20年前，我们开始研究5-羟色胺受体与神经元中cAMP的产生的关系.该受体显然具有与当时描述的其他5-HT受体（即5-HT 1、5-HT 2、5-HT 3受体）不同的药理学。我们建议将其命名为5-HT 4受体。目前，5-HT 4受体是研究最多的GPCR之一，属于“视紫红质”家族。由于存在各种各样的配体与反向激动剂，部分激动剂，激动剂和拮抗剂的档案，这种受体的药理学和生理学特性开始出现。尽管一些5-HT 4部分激动剂已经上市用于胃肠道疾病，但5-HT 4受体药物仍有待商业化用于脑疾病。然而，由于5-HT 4受体在动物模型中对记忆、抑郁和进食有公认的作用，因此仍然有希望在大脑疾病中对这个有趣的靶点进行治疗。(C)2008爱思唯尔有限公司保留所有权利。
Twenty years ago, we started the characterization of a 5-HT receptor Coupled to cAMP production in neurons. This receptor obviously had a different pharmacology to the other 5-HT receptors described at that time, i.e. the 5-HT1, 5-HT2, 5-HT3 receptors. We proposed to name it the 5-HT4 receptor. Nowadays, 5-HT4 receptors are one of the most studied GPCRs belonging to the "rhodopsin" family. Thanks to the existence of a great variety of ligands with inverse agonist, partial agonist, agonist and antagonist profiles, the pharmacological and physiological properties of this receptor are beginning to emerge. Although some 5-HT4 partial agonists have been on the market for gastro-intestinal pathologies, 5-HT4 receptor drugs have still to be commercialized for brain disorders. However, since 5-HT4 receptors have recognized effects on memory, depression and feeding in animal models, there is still hope for a therapeutic destiny of this interesting target in brain disorders. (C) 2008 Elsevier Ltd. All rights reserved.