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β受体阻滞剂与人体脂肪细胞腺苷酸环化酶

beta-blocking agents and human fat cell adenylate cyclase.

作者信息

Kather H, Simon B

出版信息

Res Commun Chem Pathol Pharmacol. 1977 Sep;18(1):11-22.

PMID:20652
Abstract

The effects of various beta-blocking agents upon the catecholamine-activated adenylate cyclase of human fat cell ghosts were studied. Both non-selective and cardio-selective beta-blocking drugs are capable in inhibiting the human enzyme system. The concentrations of the non-selective beta-blockers (bupranolol, alprenolol, propranolol, 4-hydroxypropranolol, prindolol and oxyprenolol) required to produce half maximal inhibition of isoproterenol-stimulated rates of cAMP-formation were found to be in a narrow range (5X10(-7) M-3X10(-6) M).The cardioselective beta-blocking agents, however, were only 1/100 (methypranol) to 1/1000 (atenolol, practolol) as potent as the non-selective drugs.

摘要

研究了各种β-阻滞剂对人脂肪细胞膜颗粒中儿茶酚胺激活的腺苷酸环化酶的作用。非选择性和心脏选择性β-阻滞剂均能抑制人酶系统。发现对异丙肾上腺素刺激的环磷酸腺苷(cAMP)生成速率产生半数最大抑制所需的非选择性β-阻滞剂(布普洛尔、阿普洛尔、普萘洛尔、4-羟基普萘洛尔、吲哚洛尔和氧烯洛尔)浓度在狭窄范围内(5×10⁻⁷ M - 3×10⁻⁶ M)。然而,心脏选择性β-阻滞剂的效力仅为非选择性药物的1/100(甲普洛尔)至1/1000(阿替洛尔、普拉洛尔)。

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