戊巴比妥对哺乳动物肌肉中乙酰胆碱激活通道的影响。
Effects of pentobarbitone on acetylcholine-activated channels in mammalian muscle.
作者信息
Gage P W, McKinnon D
出版信息
Br J Pharmacol. 1985 May;85(1):229-35. doi: 10.1111/j.1476-5381.1985.tb08851.x.
Abstract
Acetylcholine-activated single channel currents were recorded from the extrajunctional region of chronically denervated skeletal muscle of the rat by the patch clamp technique. In control experiments, the cumulative open-time, closed-time and burst length distributions could be well described by the sum of two exponentials. Pentobarbitone decreased the mean open time and increased the time constant of the fast component of the closed time distribution. These effects increased with drug concentration. The mean burst length was relatively independent of pentobarbitone concentration over the range of concentrations used (10-500 microM). These observations are inconsistent with a simple sequential blocking model and it is suggested that pentobarbitone has an allosteric site of action on receptor-channel complexes that makes the open state less stable.
摘要
采用膜片钳技术，从大鼠长期去神经支配的骨骼肌的接头外区域记录乙酰胆碱激活的单通道电流。在对照实验中，累积开放时间、关闭时间和爆发长度分布可用两个指数之和很好地描述。戊巴比妥降低了平均开放时间，增加了关闭时间分布快速成分的时间常数。这些效应随药物浓度增加而增强。在所使用的浓度范围（10 - 500微摩尔）内，平均爆发长度相对独立于戊巴比妥浓度。这些观察结果与简单的顺序阻断模型不一致，提示戊巴比妥在受体 - 通道复合物上有一个变构作用位点，使开放状态稳定性降低。
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