5-HT receptors linked to adenylyl cyclase activity in mammalian brain.

5-HT receptors linked to adenylyl cyclase activity in mammalian brain.
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5-HT 受体与哺乳动物大脑中的腺苷酸环化酶活性有关。

DOI:
10.1111/j.1749-6632.1990.tb16884.x
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发表时间:
1990
影响因子:
5.2
通讯作者:
Maayani,S
Maayani,S
中科院分区:
综合性期刊3区
文献类型:
--
作者:
Yocca,FD;Maayani,S

文献摘要

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5-羟色胺(5-羟色胺)膜受体,可刺激或抑制腺苷环化酶(EC 4.6。近三十年来,活动一直是众多研究的焦点。最近发表了几篇关于这一主题的综述。-3这里给出的总结着重于截至1990年6月报道的最新研究,主要集中在哺乳动物的大脑上。到目前为止,哺乳动物大脑中与腺酰环化酶相关的四种不同的5-羟色胺受体已通过药理学方法进行了阳性分类:5-羟色胺,A,4,5-羟色胺,5,5-羟色胺,6和推定的5-羟色胺受体。除了对这四种5-羟色胺受体亚型的概述外,还将深入讨论涉及特定5-羟色胺受体亚型独特方面的下列主题:1)在大鼠胚胎丘脑和豚鼠海马膜上,5-HT4受体与腺苷环化酶结合;2)在大鼠和牛的中缝背膜上,5-HTIA受体与腺酰环化酶活性明显缺乏偶联;3)与腺酰环化酶连接的5-羟色胺受体不能用目前的药物探针(孤儿受体)进行正向分类。这些主题的综述应该有助于识别和关注一些重要的问题,这些问题对于理解5-羟色胺受体/腺酰环化酶相互作用的机制是重要的。
Serotonin (5-HT) membrane receptors that either stimulate or inhibit adenylyl cyclase (EC 4.6. 1.1) activity have been a focus of numerous studies for nearly three decades. Several reviews on this subject have been published recently.’-3 The summary presented here places emphasis on recent studies reported through June, 1990, and is focused mainly on mammalian brain. To date, four distinct 5-HT receptors linked to adenylyl cyclase have been positively classified in mammalian brain by pharmacologic methods: 5-HT, A, 4 5-HT,,, 5 5-HTI,, 6 and the putative 5-HT4 receptor.’Positive classification3 designates that selective drugs are available to allow pharmacologic distinction of a particular 5-HT receptor. In addition to a general review of these four 5-HT receptor subtypes, the following topics involving unique aspects of particular 5-HT receptor subtypes will be discussed in depth: 1) the putative 5-HT4 receptor coupled to adenylyl cyclase activity in rat embryonic colliculi and guinea pig hippocampal membranes; 2) the apparent lack of coupling of the 5-HTIA receptor to adenylyl cyclase activity in rat and bovine dorsal raphe membranes and 3) 5-HT receptors linked to adenylyl cyclase which cannot be positively classified with current pharmacologic probes (“orphan” receptor^).^ The review of these topics should help identify and focus attention on some issues important for understanding the mechanisms governing 5-HT receptor/adenylyl cyclase interactions.