激动剂可阻断通过乙酰胆碱受体通道的电流。
Agonists block currents through acetylcholine receptor channels.
作者信息
Sine S M, Steinbach J H
出版信息
Biophys J. 1984 Aug;46(2):277-83. doi: 10.1016/S0006-3495(84)84022-9.
Abstract
We have examined the effects of high concentrations of cholinergic agonists on currents through single acetylcholine receptor (AChR) channels on clonal BC3H1 cells. We find that raised concentrations of acetylcholine (ACh; above 300 microM) or carbamylcholine (Carb; above 1,000 microM) produce a voltage- and concentration-dependent reduction in the mean single-channel current. Raised concentrations of suberyldicholine (Sub; above 3 microM) produce a voltage- and concentration-dependent increase in the number of brief duration low-conductance interruptions of open-channel currents. These observations can be quantitatively described by a model in which agonist molecules enter and transiently occlude the ion-channel of the AChR.
摘要
我们研究了高浓度胆碱能激动剂对克隆的BC3H1细胞上单个乙酰胆碱受体（AChR）通道电流的影响。我们发现，乙酰胆碱（ACh；高于300微摩尔）或氨甲酰胆碱（Carb；高于1000微摩尔）浓度升高会导致平均单通道电流出现电压和浓度依赖性降低。辛二酰胆碱（Sub；高于3微摩尔）浓度升高会导致开放通道电流出现短暂持续时间的低电导中断次数出现电压和浓度依赖性增加。这些观察结果可以通过一个模型进行定量描述，在该模型中，激动剂分子进入并短暂阻塞AChR的离子通道。
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