The influence of aromatic substitution on the negative inotropic action of verapamil in the isolated cat papillary muscle

Arzneimittelforschung. 1981;31(5):773-80.

Abstract

The influence of ring substitution on the negative-inotropic action of the Ca-antagonist verapamil (Isoptin) by means of qualitative and quantitative analyses of the structure-activity relationships has been investigated. The relative contribution of the two aromatic rings to the negative-inotropic potency of verapamil was tested. a) Ring substituents strongly influence the negative-inotropic potency (ED50 values from 7.9 x 10(-7) mol/l to 1.3 x 10(-4) mol/l). The character of the negative-inotropic effect typical for verapamil is not altered (except by very bulky substituents).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cats
  • Myocardial Contraction / drug effects*
  • Papillary Muscles / drug effects
  • Structure-Activity Relationship
  • Verapamil / analogs & derivatives*
  • Verapamil / pharmacology

Substances

  • Verapamil