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新型III类抗心律失常药物塞马利德对豚鼠心房肌细胞延迟整流钾电流的影响。

Effects of sematilide, a novel class III antiarrhythmic agent, on delayed rectifier K+ current in guinea pig atrial myocytes.

作者信息

Ishii Y, Muraki K, Kurihara A, Imaizumi Y, Watanabe M

机构信息

Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.

出版信息

Jpn J Pharmacol. 1996 Aug;71(4):361-5. doi: 10.1254/jjp.71.361.

Abstract

Effects of sematilide, a novel class III antiarrhythmic agent, on the delayed rectifier K+ current (Ik) were examined in guinea pig atrial myocytes using a voltage clamp technique. Sematilide inhibited both time-dependent outward current upon depolarization and tail currents (Ik-tail) at -40 mV. The concentration of sematilide required for a 50% decrease in Ik-tail was approximately 50 microM. The sematilide-sensitive current obtained using a triangular voltage command exhibited marked inward rectification and had the maximum amplitude at -30 mV. These results suggest that sematilide inhibits rapidly activating Ik in guinea pig atrial myocytes, resulting in the prolongation of action potential duration and refractoriness.

摘要

使用电压钳技术,在豚鼠心房肌细胞中研究了新型III类抗心律失常药物塞马利特对延迟整流钾电流(Ik)的影响。塞马利特抑制去极化时的时间依赖性外向电流以及 -40 mV 时的尾电流(Ik-tail)。使 Ik-tail 降低 50% 所需的塞马利特浓度约为 50 μM。使用三角电压指令获得的塞马利特敏感电流表现出明显的内向整流,并且在 -30 mV 时具有最大幅度。这些结果表明,塞马利特抑制豚鼠心房肌细胞中快速激活的 Ik,导致动作电位持续时间和不应期延长。

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