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多巴胺受体:猫脑内功能不同类型的选择性激动剂和拮抗剂。

Dopamine receptors: selective agonists and antagonists of functionally distinct types within the feline brain.

作者信息

Cools A R, Boudier A J, Rossum J M

出版信息

Eur J Pharmacol. 1976 Jun;37(2):283-93. doi: 10.1016/0014-2999(76)90036-4.

Abstract

Unilateral injections of agents that are useful tools for differentiating electrophysiologically distinct dopamine receptors within the snail Helix aspersa are given into behaviourally distinct dopamine sensitive areas within the caudate nucleus of cats. Dopamine-elicited contralateral head-turning is selectively mimicked by apomorphine and selectively inhibited by haloperidol, whereas dopamine-elicited homolateral head-turning including oro-facial dyskinesias is selectively mimicked by (3, 4-dihydroxy-phenylamino)-2-imidazoline (DPI) and selectively inhibited by ergometrine, piribedil and noradrenaline. These results indicate that the caudate nucleus of cats contains two functionally and pharmalogically distinct dopamine receptors and that Helix aspersa dopamine sensitive neurons can be used as model for the design of drugs selectively interfering with each type of receptor. The implications of these findings are considered in view of the efficacy of piribedil, L-DOPA and neuroleptics in psychomotor diseases in man.

摘要

将对区分蜗牛玛瑙螺体内电生理特性不同的多巴胺受体有用的药剂单侧注射到猫尾状核内行为特性不同的多巴胺敏感区域。多巴胺引发的对侧转头反应可被阿扑吗啡选择性模拟,并被氟哌啶醇选择性抑制;而多巴胺引发的同侧转头反应(包括口面部运动障碍)可被(3,4-二羟基苯氨基)-2-咪唑啉(DPI)选择性模拟,并被麦角新碱、匹莫齐特和去甲肾上腺素选择性抑制。这些结果表明,猫的尾状核含有两种功能和药理学特性不同的多巴胺受体,并且玛瑙螺多巴胺敏感神经元可作为设计选择性干扰每种受体类型药物的模型。鉴于匹莫齐特、左旋多巴和抗精神病药物对人类精神运动疾病的疗效,对这些发现的意义进行了探讨。

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