Antiarrhythmic properties of some 1,4-disubstituted piperazine derivatives with 伪₁-adrenoceptor affinities

详细信息    查看全文

• 作者：Monika Kubacka ; Szczepan Mogilski ; Barbara Filipek ; Henryk Marona
• 关键词：Antiarrhythmic activity ; 伪1-adrenoceptor ; Ischemia ; Piperazine derivative
• 刊名：European Journal of Pharmacology
• 出版年：15 November, 2013
• 年：2013
• 卷：720
• 期：1-3
• 页码：237-246
• 全文大小：673 K

文摘

A series of 1,4-disubstituted piperazine derivatives with 伪₁-adrenolytic properties was evaluated for antiarrhythmic, electrocardiographic and antioxidant activity in vitro and in vivo. Most of them displayed strong antiarrhythmic activity in the adrenaline induced model of arrhythmia and in the rat coronary artery ligation-reperfusion model. Their antiarrhythmic effect is mainly related to 伪₁-adrenolytic properties. Among them one compound showed characteristics similar to quinidine in different arrhythmia models as well as electrocardiogram (ECG) studies which suggests that it possesses not only 伪₁-adrenoceptor blocking properties but also affinity for cardiac Na⁺ and K⁺ channels, similar to class IA antiarrhythmic agents. Two other compounds revealed some antioxidant effects. Another compound (MH-79) is particularly promising since it displayed a strong antiarrhythmic effect without the influence on ECG record.