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中枢5-羟色胺受体:效应系统、生理作用及调节

Central serotonin receptors: effector systems, physiological roles and regulation.

作者信息

Conn P J, Sanders-Bush E

出版信息

Psychopharmacology (Berl). 1987;92(3):267-77. doi: 10.1007/BF00210830.

DOI:10.1007/BF00210830
PMID:2819915
Abstract

Radioligand binding studies have revealed four distinct serotonin (5HT) binding sites in rat brain that are thought to function as 5HT receptors. These include the 5HT-1a, 5HT-1b, 5HT-1c, and 5HT-2 binding sites. Studies have shown that the 5HT-2 binding site mediates a number of effects of 5HT agonists and serves as a 5HT receptor in neuronal and non-neuronal tissues. The 5HT-2 site employs phosphoinositide hydrolysis for signal transduction. The 5HT-1c binding site is also a functional receptor that is linked to phosphoinositide hydrolysis. However, the physiological role of the 5HT-1c receptor is not yet known. Lack of appropriate pharmacological tools for probing the 5HT-1a and 5HT-1b binding sites has made it difficult to definitively determine whether these binding sites are coupled to biochemical effector systems or mediate any of the physiological responses to 5HT agonists. However, there is some evidence that the 5HT-1a site is coupled to adenylate cyclase, and a number of functional roles for the 5HT-1a and 5HT-1b sites have been proposed.

摘要

放射性配体结合研究已揭示大鼠脑中存在四个不同的血清素(5HT)结合位点,它们被认为起着5HT受体的作用。这些位点包括5HT-1a、5HT-1b、5HT-1c和5HT-2结合位点。研究表明,5HT-2结合位点介导了5HT激动剂的多种效应,并在神经元和非神经元组织中作为5HT受体发挥作用。5HT-2位点利用磷酸肌醇水解进行信号转导。5HT-1c结合位点也是一个与磷酸肌醇水解相关的功能性受体。然而,5HT-1c受体的生理作用尚不清楚。由于缺乏合适的药理学工具来探测5HT-1a和5HT-1b结合位点,因此难以确切确定这些结合位点是否与生化效应系统偶联,或介导对5HT激动剂的任何生理反应。不过,有一些证据表明5HT-1a位点与腺苷酸环化酶偶联,并且已经提出了5HT-1a和5HT-1b位点的一些功能作用。

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Central serotonin receptors: effector systems, physiological roles and regulation.中枢5-羟色胺受体:效应系统、生理作用及调节
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2
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Phosphoinositide system-linked serotonin receptor subtypes and their pharmacological properties and clinical correlates.磷酸肌醇系统相关的5-羟色胺受体亚型及其药理学特性与临床关联
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Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1 receptor subtypes in the rat brain.抗焦虑苯氧基丙醇胺衍生物伊沙莫坦(CGP 361A)与大鼠脑中5-HT1受体亚型的相互作用。
Naunyn Schmiedebergs Arch Pharmacol. 1988 Jun;337(6):609-20. doi: 10.1007/BF00175785.
吗啡对平滑肌兴奋剂作用于豚鼠肠道的抑制作用。
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Two kinds of tryptamine receptor.两种色胺受体。
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Drugs which antagonize 5-hydroxytryptamine.拮抗5-羟色胺的药物。
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A pharmacological analysis of the mode of action of serotonin (5-hydroxytryptamine) upon the guinea-pig ileum.血清素(5-羟色胺)对豚鼠回肠作用方式的药理学分析。
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