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在局部麻醉剂存在的情况下,大鼠培养肌肉细胞单通道电流所携带的电荷。

The charge carried by single-channel currents of rat cultured muscle cells in the presence of local anaesthetics.

作者信息

Neher E

出版信息

J Physiol. 1983 Jun;339:663-78. doi: 10.1113/jphysiol.1983.sp014741.

Abstract

Acetylcholine-induced single-channel currents were measured in the presence of the lignocaine derivative QX222. Unit responses appeared as bursts of short current pulses as a result of the fast blocking action of the drug (QX222). The amplitude of the individual current pulses was not changed by the presence of the drug up to a concentration of 250 microM. The time integral of current during a burst, which for a sequential blocking model should be independent of drug concentration, decreased at concentrations of QX222 higher than 40 microM. The distribution of gap times within a burst could not be fitted by a single exponential for high concentrations of QX222. It is concluded that the simple sequential model of channel blockade does not apply for concentrations of QX222 higher than 40 microM.

摘要

在利多卡因衍生物QX222存在的情况下,测量了乙酰胆碱诱导的单通道电流。由于药物(QX222)的快速阻断作用,单位反应表现为短电流脉冲的爆发。在药物浓度高达250微摩尔时,单个电流脉冲的幅度并未因药物的存在而改变。对于顺序阻断模型而言,爆发期间电流的时间积分应与药物浓度无关,但在QX222浓度高于40微摩尔时,该积分值下降。对于高浓度的QX222,爆发内间隙时间的分布无法用单一指数拟合。得出的结论是,通道阻断的简单顺序模型不适用于高于40微摩尔的QX222浓度。

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