Two 5-HT receptors linked to adenylate cyclase in guinea pig hippocampus are discriminated by 5-carboxamidotryptamine and spiperone.
Two 5-HT receptors linked to adenylate cyclase in guinea pig hippocampus are discriminated by 5-carboxamidotryptamine and spiperone.
复制标题
豚鼠海马中与腺苷酸环化酶连接的两个 5-HT 受体可被 5-羧酰胺色胺和螺哌隆识别。
DOI：
10.1016/0014-2999(85)90408-x
复制
发表时间：
1985
影响因子：
5
通讯作者：
Green,JP
中科院分区：
文献类型：
--
作者：
Shenker,A;Maayani,S;Weinstein,H;Green,JP
对哺乳动物5-羟色胺（5-HT）受体偶联腺苷酸环化酶的药理学和生理学意义知之甚少。这些受体是否代表[3 H] 5-HT结合位点的功能相关性一直是有争议的问题（例如参见Hamon等人，1984）。我们已经开发了测量成年豚鼠海马体颗粒部分中5-HT刺激的腺苷酸环化酶活性的条件（Shenker等人，1983年a）。这种刺激是浓度依赖性的、GTP依赖性的，并且与多巴胺、㈠异丙肾上腺素和组胺引起的反应相加，表明不同的5-HT受体介导该作用;选择性5-HT拮抗剂酮色林和MDL 72222的低效力表明5-HT 2和“外周神经元”类5-HT受体都不参与该反应（Shenker等人，1983 a，B;在准备中）。几个发现，包括5-HT、色胺、5-甲氧基色胺和蟾蜍烯碱的浓度-响应曲线是浅的和非平行的事实（Shenker等人，1983 b），提出了在该系统中腺苷酸环化酶活性的刺激由5-HT受体的异质群体介导的可能性。
Relatively little is known about the pharmacology and physiological significance of mammalian 5-hydroxytryptramine (5-HT) receptors coupled to adenylate cyclase. Whether these receptors represent the functional correlate of [3H] 5-HT binding sites has been a matter of controversy (eg see Hamon et al., 1984).We have developed conditions to measure 5-HT-stimulated adenylate cyclase activity in the particulate fraction of adult guinea pig hippocampus (Shenker et al., 1983a). This stimulation is concentration-dependent, GTP-dependent, and additive to responses elicited by dopamine,(-) isoproterenol and histamine, indicating that distinct 5-HT receptors mediate the effect; the low potencies of the selective 5-HT antagonists ketanserin and MDL 72222 suggest that neither the 5-HT 2 nor the'peripheral neuronal'class of 5-HT receptor is involved in the response (Shenker et al., 1983a, b; in preparation). Several findings, including the fact that the concentration-response curves for 5-HT, tryptamine, 5-methoxytryptamine, and bufotenine are shallow and non-parallel (Shenker et al., 1983b), raised the possibility that stimulation of adenylate cyclase activity in this system was mediated by a heterogeneous population of 5-HT receptors.