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5-HT(2) Receptors.

机译:5-HT(2)受体。

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摘要

5-HT(2) receptors are G-protein coupled receptors that currently comprise three subtypes: 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. The subtypes are related in their molecular structure, amino acid sequence and signaling properties. 5-HT(2A) and 5-HT(2C) receptors have a widespread distribution and function in the central nervous system. 5-HT(2A)and 5-HT(2C) receptor antagonism is a property of certain antipsychotic and antide-pressant drugs. 5-HT(2B) receptors have a restricted expression in the central nervous system. They have an important role in embryogenesis and in the periphery. In this article, selected aspects of 5-HT(2) receptor research are reviewed for each subtype under three main headings : (i) genes, protein structure and receptor signaling; (ii) receptor localization with emphasis on the CNS and (iii) compounds. The general discussion reflects on the reasons for the limited success in the clinic of 5-HT(2) receptor subtype selective drugs.
机译:5-HT(2)受体是G蛋白偶联受体,目前包括三种亚型:5-HT(2A),5-HT(2B)和5-HT(2C)受体。亚型在它们的分子结构,氨基酸序列和信号转导特性上是相关的。 5-HT(2A)和5-HT(2C)受体在中枢神经系统中具有广泛的分布和功能。 5-HT(2A)和5-HT(2C)受体拮抗作用是某些抗精神病药和抗抑郁药的一种性质。 5-HT(2B)受体在中枢神经系统中的表达受到限制。它们在胚胎发生和外周中起重要作用。在本文中,对每种亚型的5-HT(2)受体研究的选定方面在以下三个主要标题下进行了综述:(i)基因,蛋白质结构和受体信号传导; (ii)着重于CNS和(iii)化合物的受体定位。一般性讨论反映了5-HT(2)受体亚型选择性药物在临床上取得成功的原因。

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