钠失活机制调节鱿鱼轴突中钠通道的QX-314阻断。
Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons.
作者信息
Yeh J Z
出版信息
Biophys J. 1978 Nov;24(2):569-74. doi: 10.1016/S0006-3495(78)85403-4.
Abstract
Blocking action of Na channels by QX-314, a quaternary derivative of lidocaine, was studied in internally perfused and voltage-clamped axons of squid. In axons with intact Na inactivation, QX-314 exhibited both a frequency- and a voltage-dependent block of Na channels. Repetitive pulsing to more positive potentials enhanced the degree of block. Both frequency- and voltage-dependent blocks disappeared in axons in which Na inactivation had been destroyed by either pronase or N-bromoacetamide treatment. These results support the notion that Na inactivation not only modulates the frequency-dependent block but also involves the voltage-dependent binding reaction between QX-314 and Na channels.
摘要
利多卡因的季铵衍生物QX-314对钠通道的阻断作用，在鱿鱼的内部灌注和电压钳制轴突中进行了研究。在具有完整钠失活的轴突中，QX-314表现出对钠通道的频率依赖性和电压依赖性阻断。重复刺激到更正电位会增强阻断程度。在经链霉蛋白酶或N-溴代乙酰胺处理而破坏了钠失活的轴突中，频率依赖性和电压依赖性阻断均消失。这些结果支持了这样的观点，即钠失活不仅调节频率依赖性阻断，而且涉及QX-314与钠通道之间的电压依赖性结合反应。
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