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BRL 24924:一种对非经典5-羟色胺受体有强效激动作用的物质,该受体在丘脑中的神经元中与腺苷酸环化酶正性偶联。

BRL 24924: a potent agonist at a non-classical 5-HT receptor positively coupled with adenylate cyclase in colliculi neurons.

作者信息

Dumuis A, Sebben M, Bockaert J

机构信息

Centre CNRS-INSERM de Pharmacologie-Endocrinologie, Montpellier, France.

出版信息

Eur J Pharmacol. 1989 Mar 21;162(2):381-4. doi: 10.1016/0014-2999(89)90304-x.

Abstract

A non-classical 5-hydroxytryptamine (5-HT) receptor that we have previously proposed to call 5-HT4 and which mediates stimulation of adenylate cyclase activity in mouse embryo colliculi neurons in primary culture was also stimulated by substituted benzamide derivatives such as metoclopramide and BRL 24924 ([ (+/-)-(endo)]-4-amino-5-chloro-2-methoxy-N-(1-azabicyclo-[3.3.1]-non- 4-yl)-benzamide hydrochloride). The non-additivity of the effects of 5-HT and BRL 24924 on cAMP formation and the inhibition by ICS 205 930, a potent 5-HT3 antagonist, suggest that 5-HT and BRL 24924 act on the same receptor. In light of these results, we think that a similarity may exist between the non-classical 5-HT receptor, coupled with an adenylate cyclase in colliculi neurons, and the non-classical 5-HT receptor, involved in gastric and ileum motility which is specifically stimulated by substituted benzamide derivatives in the same order of potency (metoclopramide, BRL 24924).

摘要

我们之前提议命名为5-HT4的一种非经典5-羟色胺(5-HT)受体,可介导原代培养的小鼠胚胎丘脑中神经元的腺苷酸环化酶活性的刺激作用,它也可被诸如甲氧氯普胺和BRL 24924([(±)-(内型)]-4-氨基-5-氯-2-甲氧基-N-(1-氮杂双环-[3.3.1]-壬-4-基)-苯甲酰胺盐酸盐)等取代苯甲酰胺衍生物所刺激。5-HT和BRL 24924对环磷酸腺苷(cAMP)形成的效应不存在相加性,以及强效5-HT3拮抗剂ICS 205 930的抑制作用,提示5-HT和BRL 24924作用于同一受体。鉴于这些结果,我们认为,与丘脑神经元中的腺苷酸环化酶偶联的非经典5-HT受体,和参与胃及回肠运动性、同样可被取代苯甲酰胺衍生物按相同效力顺序(甲氧氯普胺、BRL 24924)特异性刺激的非经典5-HT受体之间,可能存在相似性。

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