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替地沙米对人心房和心室纤维的细胞电生理效应。

The cellular electrophysiological effects of tedisamil in human atrial and ventricular fibers.

作者信息

Németh M, Virág L, Hála O, Varró A, Kovács G, Thormählen D, Papp J G

机构信息

Institute of Pharmacology, Albert Szent-Györgyi Medical University, Szeged, Hungary.

出版信息

Cardiovasc Res. 1996 Feb;31(2):246-8.

PMID:8730401
Abstract

The cellular electrophysiological effects of 1 microM tedisamil (KC 8857) were studied in human atrial and ventricular fibers. Conventional microelectrode technique was applied to record the transmembrane action potentials at stimulation frequency of 100 per min and 37 degrees C. Tedisamil lengthened action potential duration (APD) more in atrial than in ventricular muscle fibers; prolongation of APD90 was 28.9 +/- 3.3% (n = 6; p < 0.05) for atrial and 13.3 +/- 5.2% (n = 6; P < 0.05) for ventricular tissue. The maximal rate of depolarization was depressed slightly, but significantly by 1 microM tedisamil only in ventricular fibers (12.9 +/- 6.5%, n = 6, P < 0.05). From these cellular electrophysiological data it is concluded that the bradycardic/antiischemic agent tedisamil possesses marked Class III properties not only in cardiac tissues of experimental animals but also those of man.

摘要

研究了1微摩尔替地沙米(KC 8857)对人心房和心室纤维的细胞电生理效应。采用传统微电极技术,在37℃、每分钟100次的刺激频率下记录跨膜动作电位。替地沙米使心房肌纤维动作电位时程(APD)延长的幅度大于心室肌纤维;心房组织APD90的延长率为28.9±3.3%(n = 6;p < 0.05),心室组织为13. ± 5.2%(n = 6;P < 0.05)。仅在心室纤维中,1微摩尔替地沙米使最大去极化速率轻度但显著降低(12.9±6.5%,n = 6,P < 0.05)。从这些细胞电生理数据得出结论,心动过缓/抗缺血药物替地沙米不仅在实验动物的心脏组织中,而且在人体心脏组织中都具有明显的Ⅲ类特性。

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New pharmacological strategies for the treatment of atrial fibrillation.治疗心房颤动的新药理学策略。
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Tedisamil and lidocaine enhance each other's antiarrhythmic activity against ischaemia-induced arrhythmias in rats.替地沙米和利多卡因可增强彼此对大鼠缺血性心律失常的抗心律失常活性。
Br J Pharmacol. 2003 Aug;139(8):1389-98. doi: 10.1038/sj.bjp.0705373.
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Tedisamil and dofetilide-induced torsades de pointes, rate and potassium dependence.替地沙米和多非利特诱发的尖端扭转型室性心动过速、心率及钾依赖性。
Br J Pharmacol. 2001 Apr;132(7):1493-500. doi: 10.1038/sj.bjp.0703967.
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