普萘洛尔和儿茶酚胺与β-肾上腺素能受体的立体特异性结合。
Stereospecific binding of propranolol and catecholamines to the beta-adrenergic receptor.
作者信息
Atlas D, Steer M L, Levitzki A
出版信息
Proc Natl Acad Sci U S A. 1974 Oct;71(10):4246-8. doi: 10.1073/pnas.71.10.4246.
Abstract
The stereospecificity of the beta-adrenergic receptor of turkey erythrocyte ghosts was studied. Binding of the specific beta-adrenergic antagonist, propranolol, was found to occur exclusively with the l-stereoisomer. The stereospecificity of catecholamine binding was determined by assaying the ability of the catecholamines to displace [(3)H]propranolol. Binding of the catecholamines was also found to be stereospecific for the l-stereoisomers. Furthermore, the d-stereoisomers do not compete with the l form for binding. Using this displacement technique, we were able to calculate the dissociation constants for l-epinephrine, l-norepinephrine, and l-isoproterenol from the beta-receptor and compare these values to the apparent dissociation constants obtained from the direct activation of adenylate cyclase (EC 4.6.1.1) by these catecholamines.
摘要
研究了火鸡红细胞膜的β-肾上腺素能受体的立体特异性。发现特异性β-肾上腺素能拮抗剂普萘洛尔仅与l-立体异构体结合。通过测定儿茶酚胺取代[(3)H]普萘洛尔的能力来确定儿茶酚胺结合的立体特异性。还发现儿茶酚胺的结合对l-立体异构体具有立体特异性。此外，d-立体异构体不与l-形式竞争结合。使用这种取代技术，我们能够计算l-肾上腺素、l-去甲肾上腺素和l-异丙肾上腺素与β-受体的解离常数，并将这些值与通过这些儿茶酚胺直接激活腺苷酸环化酶（EC 4.6.1.1）获得的表观解离常数进行比较。
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