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β-肾上腺素受体阻断剂的疏水性与非特异性药理作用之间的相关性

Correlations between hydrophobicity and non-specific pharmacological effects of beta-adrenoceptor blocking agents.

作者信息

Hellenbrecht D, Gortner L

出版信息

Pol J Pharmacol Pharm. 1976 Nov-Dec;28(6):625-30.

PMID:13353
Abstract

It was the aim of this study to test whether the non-specific pharmacological activities of the beta-adrenergic blocking drugs can be predicted by estimation of the hydrophobicity of the compounds. Srong correlations were obtained between the octanol buffer partition coefficients and the ability of the drugs to decrease conduction velocity of the isolated frog heart, to raise the electrically induced ventricular fibrillation threshold in guinea pigs, and to depress ventricular contractility in the cat. The strong correlations between the partition coefficients and the pharmacological actions suggest that estimation of the hydrophobicity of the beta-adrenergic blocking drugs is suitable to predict the non-specific pharmacological properties.

摘要

本研究的目的是测试β-肾上腺素能阻断药物的非特异性药理活性是否可以通过估计化合物的疏水性来预测。在辛醇缓冲液分配系数与药物降低离体蛙心传导速度、提高豚鼠电诱导室颤阈值以及抑制猫心室收缩力的能力之间获得了强相关性。分配系数与药理作用之间的强相关性表明,估计β-肾上腺素能阻断药物的疏水性适合于预测其非特异性药理特性。

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