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