Gurbanov K G, Paperno A A, Spasov A A, Vasil'ev P M, Breslaukhov A G, Luk'ianenko N G, Basok S S, Kulygina E Iu, Bogashchenko T Iu
Eksp Klin Farmakol. 1993 May-Jun;56(3):32-4.
The relationship between the inotropic effect and chemical structure of 15-crown-5 and 18-crown-6 derivatives was studied in experiments in open-chest anaesthesized cats, by using computer-aided analysis. The findings showed that the 15-crown-5 derivatives produced more pronounced cardiotropic effect and they were less toxic than 18-crown-6 derivatives. Computer-aided analysis revealed pharmacophoric groups which are responsible for cardiotropic (negative inotropic) activity in the series of crown ether derivatives.
在开胸麻醉猫的实验中,采用计算机辅助分析方法研究了15-冠-5和18-冠-6衍生物的变力作用与化学结构之间的关系。研究结果表明,15-冠-5衍生物产生更明显的心脏otropic效应,且其毒性低于18-冠-6衍生物。计算机辅助分析揭示了冠醚衍生物系列中负责心脏otropic(负性变力)活性的药效基团。