芳香取代对维拉帕米在离体猫乳头肌中负性肌力作用的影响。
The influence of aromatic substitution on the negative inotropic action of verapamil in the isolated cat papillary muscle.
作者信息
Mannhold R, Zierden P, Bayer R, Rodenkirchen R, Steiner R
出版信息
Arzneimittelforschung. 1981;31(5):773-80.
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).
通过对构效关系进行定性和定量分析，研究了环取代对钙拮抗剂维拉帕米（异搏定）负性肌力作用的影响。测试了两个芳香环对维拉帕米负性肌力效能的相对贡献。a）环取代基强烈影响负性肌力效能（ED50值从7.9×10⁻⁷mol/l至1.3×10⁻⁴mol/l）。维拉帕米典型的负性肌力作用特性未改变（非常大的取代基除外）。
Zotero 插件