新型化合物CERM 11956与苄普地尔和硝苯地平在离体豚鼠心脏中的抗缺血活性比较。

The anti-ischaemic activity of the novel compound, CERM 11956, compared with that of bepridil and nifedipine in isolated guinea-pig hearts.

作者信息

Boddeke E W, Wilffert B, Heynis J B, Hugtenburg J G, Jap W T, Veldsema-Currie R D, Van Zwieten P A

机构信息

Division of Pharmacotherapy/Pharmacology, University of Amsterdam, The Netherlands.

出版信息

Eur J Pharmacol. 1988 May 10;149(3):195-203. doi: 10.1016/0014-2999(88)90649-8.

DOI:10.1016/0014-2999(88)90649-8

PMID:3261692

Abstract

A comparison between the protective activity of bepridil, its novel derivative, CERM 11956, and nifedipine in isolated electrically paced guinea-pig hearts after 60 min of global ischaemia followed by 30 min of reperfusion has been made. All three compounds exerted a significant anti-ischaemic effect, as indicated by an improved recovery of functional parameters (left ventricular pressure and coronary perfusion), a delayed onset of the ischaemic contracture, and an enhanced recovery of biochemical (CrP, ATP and adenylate energy charge) parameters. The most pronounced anti-ischaemic activity was shown by the compound CERM 11956 at concentrations that displayed only minor negative inotropic activity. From the results it may be concluded that the new bepridil derivative, CERM 11956, is a promising and potent anti-ischaemic compound, which has little influence on haemodynamic parameters.

摘要

比较了苄普地尔及其新型衍生物CERM 11956与硝苯地平在离体电刺激豚鼠心脏上的保护活性，先进行60分钟全心缺血，再进行30分钟再灌注。所有三种化合物均发挥了显著的抗缺血作用，表现为功能参数（左心室压力和冠状动脉灌注）恢复改善、缺血性挛缩延迟出现以及生化参数（磷酸肌酸、三磷酸腺苷和腺苷酸能荷）恢复增强。化合物CERM 11956在仅表现出轻微负性肌力活性的浓度下显示出最显著的抗缺血活性。从结果可以得出结论，新型苄普地尔衍生物CERM 11956是一种有前景的强效抗缺血化合物，对血流动力学参数影响很小。