阻断钠/钙交换的氨氯地平衍生物可抑制钠负荷心肌细胞中的自发性内向电流。

Amiloride derivatives that block Na+/Ca2+ exchange inhibit spontaneous inward currents in Na+-loaded cardiac myocytes.

作者信息

Cragoe E, Ravens U, Wettwer E

出版信息

Eur J Pharmacol. 1987 Aug 4;140(1):113-6. doi: 10.1016/0014-2999(87)90642-x.

PMID:2442010

Abstract

Spontaneous electrical and mechanical activity was observed when single myocytes from guinea-pig hearts were loaded with sodium by direct intracellular application. Transient membrane depolarizations were found to be due to spontaneous inward currents (Isp). Both Isp and spontaneous contractions were abolished by 2',3'-benzobenzamil or 3',4'-dichlorobenzamil, two compounds that were previously reported to inhibit Na+/Ca2+ exchange. These findings suggest that the spontaneous membrane currents in Na+-loaded myocytes could be generated by the Na+/Ca2+ exchange mechanism.

摘要

当通过直接细胞内给药使豚鼠心脏的单个心肌细胞负载钠时，观察到自发的电活动和机械活动。发现瞬时膜去极化是由于自发内向电流（Isp）所致。Isp和自发收缩均被2'，3'-苯并苯甲酰胺或3'，4'-二氯苯甲酰胺消除，这两种化合物先前报道可抑制Na+/Ca2+交换。这些发现表明，负载钠的心肌细胞中的自发膜电流可能由Na+/Ca2+交换机制产生。