Pharmacological classification of adrenergic α receptors in the guinea pig
Pharmacological classification of adrenergic α receptors in the guinea pig
复制标题
豚鼠肾上腺素α受体的药理学分类
作者：
J. Wikberg
一段时间以来，拟交感胺的作用引起了人们的广泛关注。 Ahlquist1-3 引入了肾上腺素能 α 和 β 受体的概念来解释其中一些胺对不同器官系统的影响的差异，然后 Lands 等人 4,5 提出存在两种类型的 β 受体：β1 和 β2。有人声称肾上腺素能神经元的 α 受体与平滑肌的 α 受体之间存在药理学差异6-9。我之前已经证明，豚鼠回肠胆碱能神经元的抑制性α受体在药理学上与位于豚鼠回盲部括约肌和兔主动脉平滑肌中的兴奋性α受体不同10-13。 Langer14 提出有两种 α 受体：α1 和 α2（另见参考文献 15）。采用这种命名法，有人提出，当去氧肾上腺素与受体的相对亲和力强于可乐定时，则存在α1受体；当相对亲和力相反时，则存在α2受体13，因此表明兔主动脉和肺动脉的平滑肌细胞以及豚鼠回盲部括约肌中存在α1受体；豚鼠回肠的胆碱能神经元以及兔肺动脉和大鼠输精管的肾上腺素能神经元中的抑制性α2受体。我在此报告支持两种 α 受体理论的进一步研究结果。
THE actions of sympathomimetic amines have attracted considerable attention for some time. Ahlquist1–3 introduced the concept of adrenergic α and β receptors to explain the differences in the effects of some of these amines on various organ systems and then Lands et al.4,5 suggested the existence of two types of β receptors, β1 and β2. It has been claimed that there is a pharmacological difference between α receptors at adrenergic neurones and those in smooth muscle6–9. I have previously shown that the inhibitory α receptor of the cholinergic neurone in guinea pig ileum is pharmacologically different from the excitatory α receptor located in the smooth muscle of the guinea pig ileocaecal sphincter and rabbit aorta10–13. Langer14 suggested that there are two kinds of α receptors, α1 and α2 (see also ref. 15). Adopting this nomenclature, it was proposed that α1 receptors are present when the relative affinity of phenylephrine for the receptors is stronger than that of clonidine, and α2 receptors when the relative affinities are reversed13, α1 Receptors have thus been shown to be present in smooth muscle cells of rabbit aorta and pulmonary artery, and in guinea pig ileocaecal sphincter; and inhibitory α2 receptors in cholinergic neurones of guinea pig ileum and in adrenergic neurones of rabbit pulmonary artery and rat vas deferens. I report here the results of further studies supporting the theory of two types of α receptors.