Varro A, Nakaya Y, Elharrar V, Surawicz B
Eur J Pharmacol. 1985 Jun 19;112(3):419-22. doi: 10.1016/0014-2999(85)90791-5.
Superfusion with 5 micrograms/ml amiodarone for 3-4 h induced use-dependent Vmax block in dog Purkinje and guinea pig ventricular muscle fibers. The recovery from block was exponential with tau of 289 +/- 30 ms in Purkinje (n = 7) and 282 +/- 47 ms in muscle (n = 6) fibers. The onset of frequency-dependent Vmax block was rapid, i.e. reached steady state after 4.2 +/- 0.5 beats (n = 5). The combination of rapid interaction with sodium channel and the reported action potential lengthening make amiodarone unique among Class I antiarrhythmic drugs.
用5微克/毫升胺碘酮超灌流3 - 4小时可在犬浦肯野纤维和豚鼠心室肌纤维中诱导出使用依赖性Vmax阻滞。阻滞的恢复呈指数形式,浦肯野纤维(n = 7)的τ为289±30毫秒,肌纤维(n = 6)的τ为282±47毫秒。频率依赖性Vmax阻滞的起效迅速,即在4.2±0.5次搏动后达到稳态(n = 5)。与钠通道的快速相互作用以及所报道的动作电位延长相结合,使胺碘酮在I类抗心律失常药物中独树一帜。