关于阿福唑嗪抗纤颤作用的机制。

On the mechanism of antifibrillatory effect of afobazole.

作者信息

Kryzhanovskyi S A, Stolyaruck V N, Vititnova M B, Tsorin I B, Seredenin S B

机构信息

V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia.

出版信息

Bull Exp Biol Med. 2010 Sep;149(3):314-7. doi: 10.1007/s10517-010-0935-y.

DOI:10.1007/s10517-010-0935-y

PMID:21246090

Abstract

Effect of afobazole on the threshold of electrical fibrillation of the heart was studied on anesthetized rats with intact myocardium. It was shown that the drug considerably increased the threshold of electrical fibrillation of the heart, being not inferior to reference class I antiarrhythmic drugs (lidocaine and procainamide) according to V. Williamse classification. Against the background of preliminary injection of σ-receptor antagonist haloperidol, afobazole exhibited no antifibrillatory activity. These findings and analysis of published reports suggest that antifibrillatory activity of afobazole is determined by its antagonistic influence on σ1-receptors localized in cardiomyocyte cytosol.

摘要

在心肌完整的麻醉大鼠身上研究了阿福唑嗪对心脏电致纤颤阈值的影响。结果表明，该药显著提高了心脏电致纤颤阈值，根据V. Williamse分类，其效果不低于参考的I类抗心律失常药物（利多卡因和普鲁卡因酰胺）。在预先注射σ受体拮抗剂氟哌啶醇的背景下，阿福唑嗪未表现出抗纤颤活性。这些发现以及对已发表报告的分析表明，阿福唑嗪的抗纤颤活性取决于其对位于心肌细胞质中的σ1受体的拮抗作用。