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吗啡与磷脂酰丝氨酸的立体特异性结合。

Stereospecific binding of morphine to phosphatidyl serine.

作者信息

Abood L G, Host W P

出版信息

Psychopharmacol Commun. 1975;1(1):29-35.

PMID:1241450
Abstract

By measuring the adsorption of 14C-morphine to a surface film at an air-water interface, it was shown that morphine binds to phosphatidyl serine in a 1:1 molar ratio. With the use of levorphanol and the inactive d-isomer, dextrorphan, it could be demonstrated that the interaction was stereospecific. A Lineweaver-Burk plot disclosed that levorphanol and morphine competitively interacted with the lipid; the Km for morphine was 1.6 X 10(-5)M and the Ki for levorphanol was 4.8 X 10(-5)M. Heroin, a stronger opiate, had a greater affinity for phosphatidyl serine than did morphine or levorphanol.

摘要

通过测量14C-吗啡在气-水界面处对表面膜的吸附,结果表明吗啡以1:1的摩尔比与磷脂酰丝氨酸结合。使用左啡诺和无活性的d-异构体右啡烷,可以证明这种相互作用具有立体特异性。双倒数作图表明左啡诺和吗啡与脂质发生竞争性相互作用;吗啡的米氏常数(Km)为1.6×10^(-5)M,左啡诺的抑制常数(Ki)为4.8×10^(-5)M。海洛因作为一种更强效的阿片类药物,对磷脂酰丝氨酸的亲和力比吗啡或左啡诺更高。

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