CHANG V, RAND M J
Br J Pharmacol Chemother. 1960 Dec;15(4):588-600. doi: 10.1111/j.1476-5381.1960.tb00287.x.
It has been shown by others that hemicholinium (alpha,alpha'-dimethylethanolamino-4,4'-biacetophenone) inhibits the synthesis of acetylcholine, an effect which is reversed by choline. Hemicholinium produces a failure of response to nerve stimulation in the following sympathetically innervated preparations: guinea-pig isolated vas deferens, rabbit isolated uterus, rabbit isolated colon, perfused rabbit ear, cat isolated atria and the piloerector muscles in the cat's tail. The blocking action of hemicholinium on the responses to postganglionic sympathetic stimulation resembles its blocking action against cholinergic nerve stimulation observed on rabbit isolated atria with vagus nerves, rabbit isolated vagina with pelvic nerves, and guinea-pig isolated diaphragm with phrenic nerve. The failure of transmission produced by hemicholinium in sympathetic nerves and in cholinergic nerves can be reversed by choline. It is suggested that if there were a cholinergic junction at sympathetic nerve endings the mechanism of the blocking action of hemicholinium at these endings could be explained by inhibition of acetylcholine synthesis.
其他人已证明，半胆碱（α，α'-二甲基乙醇氨基-4,4'-二乙酰苯）可抑制乙酰胆碱的合成，胆碱可逆转这一效应。半胆碱在以下交感神经支配的制剂中会导致对神经刺激的反应失效：豚鼠离体输精管、兔离体子宫、兔离体结肠、灌注兔耳、猫离体心房以及猫尾巴上的竖毛肌。半胆碱对节后交感神经刺激反应的阻断作用，类似于其对兔离体心房伴迷走神经、兔离体阴道伴盆神经以及豚鼠离体膈肌伴膈神经的胆碱能神经刺激的阻断作用。半胆碱在交感神经和胆碱能神经中产生的传递失效可被胆碱逆转。有人提出，如果交感神经末梢存在胆碱能接头，那么半胆碱在这些末梢的阻断作用机制可以用抑制乙酰胆碱合成来解释。
