Skliarov A I, Lavrent'eva V V
Zh Evol Biokhim Fiziol. 1987 May-Jun;23(3):314-20.
The effect of 13 acetylcholine and tetramethylammonium derivatives on cholinoreceptors of isolated neurone on the pond snail has been investigated by the analysis of membrane current fluctuations at 10 and 20 degrees C. The elementary current was independent from the agonist structure. The channel open time and its Q10 coefficient were found to be maximum for acetylcholine. At low concentrations, acetylcholine derivative with four groups in its methylene chain exhibited the weakest activity. Agonist activity at higher concentrations was evaluated by maximum increase in the membrane current. With respect to this character, the derivative with two ethyl radicals in its cation group was found to be the weakest one. Possible causes of low activities of the agonists studied in comparison with that of acetylcholine are discussed.
通过分析在10摄氏度和20摄氏度下分离的池塘蜗牛神经元膜电流波动，研究了13种乙酰胆碱和四甲基铵衍生物对其胆碱受体的影响。基本电流与激动剂结构无关。发现乙酰胆碱的通道开放时间及其Q10系数最大。在低浓度下，亚甲基链中有四个基团的乙酰胆碱衍生物表现出最弱的活性。通过膜电流的最大增加来评估较高浓度下的激动剂活性。就这一特性而言，阳离子基团中有两个乙基的衍生物是最弱的。讨论了与乙酰胆碱相比所研究的激动剂活性较低的可能原因。
