Ahlquist R P
Fed Proc. 1977 Nov;36(12):2572-4.
Drug receptors are usually defined in terms of specific agonists and blocking agents. The adrenoreceptor occurs in two forms, alpha and beta. From a pharmacologic point of view, this receptor concept has proved useful by allowing the development of new, selective agonists and blocking agents. From a physiologic viewpoint, there is no need for two receptors. Clinically, it is important to find out whether the pharmacologic adrenoceptors are immutable. Evidence is accumulating, both pro and con, regarding this point. Some of the effects of temperature on the response of the isolated dilator muscle of the rabbit iris to catecholamines are described. The following questions are asked: Is it not possible that there is only one adrenoceptor whose specific agonists are epinephrine or norepinephrine? Do the alpha and beta configuration depend only on the local environment? While no answers are given, it is concluded that these are clinically relavant questions.
药物受体通常根据特定的激动剂和阻断剂来定义。肾上腺素能受体有两种形式,α和β。从药理学角度来看,这种受体概念已被证明是有用的,它使得新型选择性激动剂和阻断剂得以开发。从生理学观点来看,并不需要两种受体。临床上,弄清楚药理学上的肾上腺素能受体是否一成不变很重要。关于这一点,正反两方面的证据都在不断积累。本文描述了温度对家兔虹膜离体扩约肌对儿茶酚胺反应的一些影响。文中提出了以下问题:有没有可能只存在一种肾上腺素能受体,其特定激动剂是肾上腺素或去甲肾上腺素?α和β构型是否仅取决于局部环境?虽然未给出答案,但得出的结论是,这些都是临床上相关的问题。