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

Quantitative structure-activity relationships (QSAR) in bradykinin ant agonists with activity on rat uterus and/or guinea pig ileum were inve stigated by the Free-Wilson method in the Fujita-Ban approach. The sub stituent contributions to antagonist activity were calculated by multi ple linear regression. The used QSAR model adequately describes the ex perimental data, so that the assumption about additivity and independe nce of the substituent contributions to the overall activity is valid. The obtained results allow a survey of the effect of different modifi cations on the antagonist potency. Information about the influence of various substitutions on the selectivity of the antagonists can be ext racted from the comparison of the QSAR for bath the tissues studied.