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心脏毒蕈碱受体亚型的药理学证据。

Pharmacological evidence for cardiac muscarinic receptor subtypes.

作者信息

Chassaing C, Dureng G, Baissat J, Duchêne-Marullaz P

出版信息

Life Sci. 1984 Oct 22;35(17):1739-45. doi: 10.1016/0024-3205(84)90270-4.

Abstract

The chronotropic and inotropic effects of muscarinic receptor agonists (Acetylcholine, Arecoline, Carbachol, Furtrethonium) and antagonists (Atropine, N-methyl and N-butyl scopolammonium, pirenzepine) on isolated guinea-pig atria were studied. All had a greater affinity constants for muscarinic receptors as assessed in terms of inotropic effects than in terms of chronotropic effects. This difference, well correlated with the pharmacological effect, suggests the occurrence of cardiac muscarinic receptor subtypes, one mediating heart rate and the other contractile force. The ratio of chronotropic to inotropic potencies for each agent shows that the physiological mediator. Acetylcholine, differentiates best between the two subtypes, while atropine is the least discriminatory.

摘要

研究了毒蕈碱受体激动剂(乙酰胆碱、槟榔碱、卡巴胆碱、醋甲胆碱)和拮抗剂(阿托品、N-甲基和N-丁基东莨菪碱、哌仑西平)对离体豚鼠心房的变时性和变力性作用。就变力作用而言,所有药物对毒蕈碱受体的亲和力常数均大于变时作用方面的亲和力常数。这种差异与药理效应密切相关,提示存在心脏毒蕈碱受体亚型,一种介导心率,另一种介导收缩力。每种药物的变时效力与变力效力之比表明,生理性介质乙酰胆碱对两种亚型的区分最佳,而阿托品的区分能力最差。

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