FRANK G B
Br J Pharmacol Chemother. 1961 Aug;17(1):59-69. doi: 10.1111/j.1476-5381.1961.tb01104.x.
The sensitivity of completely denervated and the innervated end-plate regions of partially denervated frog's sartorius muscles to stimulation by drugs has been investigated. The drugs were tested on muscles isolated 12 to 39 days following denervation. On the basis of the results obtained most of the drugs could be put into one of two main groups. The first group included choline, tetramethylammonium, carbachol and decamethonium; these drugs readily stimulated non-denervated muscles, and chronic denervation, either partial or complete, greatly increased the sensitivity of the muscles. The second group included pilocarpine and carbamate of (2-hydroxypropyl) trimethyl ammonium chloride (Bethanechol, U.S.P.). The muscles were relatively insensitive to stimulation by these two drugs. They could stimulate the muscles if applied in high enough concentrations, but the responses thus obtained could not be distinguished from responses produced by similar concentrations of sucrose and chronic denervation did not increase the sensitivity of the muscles to stimulation by these two drugs. Methacholine, like the drugs in the second group, was unable to stimulate the muscles in low concentrations, but chronic denervation rendered the muscles sensitive to stimulation by this drug. Tetraethylammonium presented a completely different pattern of activity which was consistent with a hypothesis that in low doses this drug stimulates skeletal muscle by causing a release of acetylcholine from nerve endings in the muscle.
对完全去神经支配以及部分去神经支配的青蛙缝匠肌中去神经支配和有神经支配的终板区域对药物刺激的敏感性进行了研究。在去神经支配后12至39天分离出的肌肉上对这些药物进行了测试。根据所获得的结果，大多数药物可分为两个主要类别之一。第一类包括胆碱、四甲铵、卡巴胆碱和十烃季铵；这些药物能轻易刺激未去神经支配的肌肉，而无论是部分还是完全的慢性去神经支配都会大大增加肌肉的敏感性。第二类包括毛果芸香碱和（2-羟丙基）三甲基氯化铵的氨基甲酸盐（乌拉胆碱，美国药典）。肌肉对这两种药物的刺激相对不敏感。如果以足够高的浓度应用，它们能刺激肌肉，但由此获得的反应与相似浓度蔗糖产生的反应无法区分，并且慢性去神经支配并未增加肌肉对这两种药物刺激的敏感性。乙酰甲胆碱与第二类药物一样，在低浓度时无法刺激肌肉，但慢性去神经支配使肌肉对该药物的刺激敏感。四乙铵呈现出完全不同的活性模式，这与一种假设一致，即低剂量时该药物通过促使肌肉神经末梢释放乙酰胆碱来刺激骨骼肌。
