块心脏钠离子通道的研究胺碘酮通过Vmax单心室细胞的动作电位。

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我Kodama Honjo H, Kamiya K,富山J

块心脏钠离子通道的研究胺碘酮通过Vmax单心室细胞的动作电位。

Br J杂志。1991年3月,102 (3):651 - 6。doi: 10.1111 / j.1476-5381.1991.tb12228.x。

PubMed ID

1364834 (在PubMed

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文摘

1。急性胺碘酮对心脏的影响钠离子通道研究从豚鼠心脏心室细胞分离,并与利多卡因。2。跨膜电位是由全细胞记录和控制current-clamp和电压钳分别通过吸液管电极。的最大的一击速度(Vmax)动作电位被用作质量指标的钠离子通道的可用性。3所示。在细胞用胺碘酮治疗(1 microM)或利多卡因(40 microM),参考Vmax动作电位引起在0.03赫兹下降了6 - 11%,表明最小主音块钠离子通道。4所示。应用程序的一个调节这些细胞去极化导致显著降低Vmax后续测试动作电位。Vmax减少在一个指数函数作为增强夹脉冲持续时间延长。 Time constants at 0 mV clamp were 25 ms for amiodarone and 122 ms for lignocaine. 5. Vmax recovery of test action potential following a 1000 ms 0 mV clamp was approximated by a dual exponential function. Time constants for the late slow component (tau R) at the resting potential level were 418 ms for amiodarone and 178 ms for lignocaine. tau R values were shortened in a voltage-dependent manner by hyperpolarization during the coupling interval. 6. These findings suggested that amiodarone, like lignocaine, blocks the sodium channel primarily when it is in the inactivated state. Both onset and offset kinetics of the block are very rapid. Such sodium channel blocking characteristics may contribute to its potent antiarrhythmic activity.

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药物

胺碘酮