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Study of the interaction of sulfur dioxide derivative with cardiac sodium channel

机译:二氧化硫衍生物与心脏钠通道相互作用的研究

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摘要

The effects of sulfur dioxide (SO2) derivatives (bisulfite and sulfite, 1:3 M/M) on voltage-dependent sodium channel in isolated rat ventricular myocyte were studied using the whole cell patch-clamp technique. SO2 derivatives increased sodium current (I-Na) in a concentration-dependent manner. SO2 derivatives at 10 mu M significantly shifted steady-state inactivation curve Of I-Na to more positive potentials, but did not affect the activation curve. SO2 derivatives markedly shifted the curve of time-dependent recovery of IN. from inactivation to the left, and accelerated the recovery of I-Na. SO2 derivatives also significantly shortened the activation and inactivation time constants of I-Na. These results indicated that SO2 derivatives produced concentration-dependent stimulation of cardiac sodium channels, which due mainly to the interaction of the drug with sodium channels in the inactivated state. (c) 2005 Elsevier B.V. All rights reserved.
机译:使用全细胞膜片钳技术研究了二氧化硫(SO2)衍生物(亚硫酸氢盐和亚硫酸盐,1:3 M / M)对离体大鼠心室肌细胞中电压依赖性钠通道的影响。 SO2衍生物以浓度依赖性方式增加钠电流(I-Na)。 10μM的SO2衍生物将I-Na的稳态失活曲线显着转移到更多的正电势,但不影响活化曲线。 SO2衍生物显着改变了IN的时间依赖性恢复曲线。从灭活到左侧,并加速了I-Na的恢复。 SO 2衍生物也显着缩短了I-Na的活化和失活时间常数。这些结果表明,SO 2衍生物产生浓度依赖性的心脏钠通道刺激,这主要是由于药物与灭活状态下的钠通道相互作用。 (c)2005 Elsevier B.V.保留所有权利。

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