QSAR IN BRADYKININ ANTAGONISTS - INHIBITION OF THE BRADYKININ-INDUCED CONTRACTION OF THE ISOLATED RAT UTERUS AND GUINEA-PIG ILEUM

被引：3

作者：

DECASTRO, LFP

REISSMANN, S

机构：

[1] Institute of Biochemistry and Biophysics, Faculty of Biology and Pharmacology, Friedrich-Schiller University, Jena, 07743

来源：

QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS | 1995年 / 14卷 / 03期

关键词：

ANTAGONIST; BRADYKININ; FREE-WILSON METHOD;

D O I：

10.1002/qsar.19950140304

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quantitative structure-activity relationships (QSAR) in bradykinin antagonists with activity on rat uterus and/or guinea pig ileum were investigated by the Free-Wilson method in the Fujita-Ban approach. The substituent contributions to antagonist activity were calculated by multiple linear regression. The used QSAR model adequately describes the experimental data, so that the assumption about additivity and independence of the substituent contributions to the overall activity is valid. The obtained results allow a survey of the effect of different modifications on the antagonist potency. Information about the influence of various substitutions on the selectivity of the antagonists can be extracted from the comparison of the QSAR for bath the tissues studied.

引用

页码：249 / 257

页数：9

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