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[胆碱能受体立体选择性的比较研究]

[A comparative study of the stereoselectivity of cholinoreceptors].

作者信息

Mikhel'son M Ia, Kolganova O I, Lukomskaia N Ia, Protas L L, Sokolov G P

出版信息

Zh Evol Biokhim Fiziol. 1979 Jan-Feb;15(1):42-7.

PMID:95838
Abstract

Muscarine-sensitive cholinoreceptors (M-ChR) of higher vertebrates exhibit high stereoselectivity which is also revealed with respect to enantiomers of a very potent muscarinomimetic methyldilvasen (F-2268), the stereospecific index (SSI) being about 100. M-ChRs in the neuronal membrane of the gastropod mollusc Planorbarius corneus and in the hearts of the bivalve molluscs Mercenaria stimpsoni and Anadara broughtoni are highly sensitive to methyldilvasen (10(-9)-10(-10) M), but their sensitivity to its enantiomers is identical. In heart atria of the tortoise Testudo horsfieldi, frog Rana temporaria, and fishes Siluris glanis, Cyprinus carpio, as well as in ventricles of tadpoles, high SSI was revealed. These data are consistent with a hypothesis that during evolution of vertebrates no significant changes took place in the active center of M-ChR. Possibly, the lack of stereoselectivity in the investigated molluscan M-ChRs, together with their other peculiarities (they are not blocked by atropine), indicate "immaturity" of these receptors.

摘要

高等脊椎动物的毒蕈碱敏感胆碱能受体(M - ChR)表现出高度的立体选择性,这在一种非常有效的拟毒蕈碱药物甲基地尔维辛(F - 2268)的对映体方面也有所体现,其立体特异性指数(SSI)约为100。腹足纲软体动物角田螺神经元膜以及双壳纲软体动物史氏篮子蛤和布氏蚶心脏中的M - ChRs对甲基地尔维辛高度敏感(10⁻⁹ - 10⁻¹⁰ M),但它们对其对映体的敏感性相同。在陆龟赫曼陆龟、青蛙欧洲林蛙以及鱼类鲶鱼、鲤鱼的心房,以及蝌蚪的心室中,发现了较高的SSI。这些数据与一个假设一致,即在脊椎动物进化过程中,M - ChR的活性中心没有发生显著变化。可能,所研究的软体动物M - ChRs缺乏立体选择性,以及它们的其他特性(它们不受阿托品阻断),表明这些受体“不成熟”。

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