KATZ B, THESLEFF S
Br J Pharmacol Chemother. 1957 Jun;12(2):260-4. doi: 10.1111/j.1476-5381.1957.tb00131.x.
The effect of edrophonium (3-hydroxy-phenyl-dimethylethylammonium chloride) on the motor end-plate and its interaction with acetylcholine and carbachol has been investigated. Use was made of intracellular recording of membrane potential and of ionophoretic micro-application of drugs from single and twin-pipettes.Small doses of edrophonium potentiate the depolarizing effect of acetylcholine, but not that of carbachol. This action can be observed with doses of edrophonium which have no depolarizing effect by themselves. Large doses of edrophonium have some depolarizing action and, at the same time, inhibit depolarizations produced by carbachol. After treatment with neostigmine, edrophonium fails to potentiate the acetylcholine response. The observations are in agreement with the view that the principal action of edrophonium on the neuromuscular junction is that of a potent and rapidly acting anticholinesterase.
研究了依酚氯铵(3-羟基苯基二甲基乙基氯化铵)对运动终板的作用及其与乙酰胆碱和卡巴胆碱的相互作用。采用细胞内记录膜电位以及通过单管和双管离子电泳微量给药的方法。小剂量的依酚氯铵可增强乙酰胆碱的去极化作用,但对卡巴胆碱则无此作用。自身无去极化作用的依酚氯铵剂量即可观察到这种作用。大剂量的依酚氯铵有一定的去极化作用,同时抑制卡巴胆碱引起的去极化。用新斯的明处理后,依酚氯铵不能增强乙酰胆碱反应。这些观察结果与依酚氯铵在神经肌肉接头处的主要作用是强效且快速起效的抗胆碱酯酶这一观点相符。