Moritoki H, Ishida Y
Eur J Pharmacol. 1977 Apr 21;42(4):347-54. doi: 10.1016/0014-2999(77)90168-6.
Acetate esters, such as aspirin methylester, aspirin and resorcinol monoacetate, induced contractions of guinea-pig ileum. Their actions were selectively antagonized by atropine, but were not affected by ganglion blocking agents, conduction blockers, aging with cooling, anoxia or antihistaminics. On the other hand, N-acetates, such as acetanilide and p-acetaminophenol, and no contractile action on the ileum. These acetate esters thus seemed to have a cholinergic action, and not a direct action on muscle or other known specific receptors for endogenous active substances. The contractions induced by the acetate esters were selectively potentiated by low concentrations of choline, whereas those induced by acetylcholine, nicotine, 5-hydroxytryptamine and histamine were not. However, N-acetates did not induce the contractions even in the presence of choline. Organophosphorus cholinesterase inhibitors, such as diisopropyl fluorophosphate and paraoxon, selectively and irreversibly inhibited the actions of aspirin and N,O-diacetyl-p-aminophenol with or without choline. From these results, it is concluded that the acetate esters with or without choline act through the cholinergic system. However, their actions cannot be explained in terms of known mechanisms, such as acetylcholine release, cholinesterase inhibition or a direct muscarinic action. Therefore, the acetate esters, including phenyl acetate which was supposed to be a releaser of acetylcholine, seem to have a hitherto undescribed type of cholinergic action whose mechanism is unknown. It seems that organophosphate-sensitive esterase(s) in the preparation may be essential for initiation of the actions of the acetate esters with or without choline, but the mechanism of the effect of choline is unknown.
醋酸酯，如阿司匹林甲酯、阿司匹林和间苯二酚单醋酸酯，可引起豚鼠回肠收缩。它们的作用可被阿托品选择性拮抗，但不受神经节阻断剂、传导阻滞剂、冷却老化、缺氧或抗组胺药的影响。另一方面，N - 醋酸酯，如乙酰苯胺和对乙酰氨基酚，对回肠无收缩作用。因此，这些醋酸酯似乎具有胆碱能作用，而不是对肌肉或其他已知内源性活性物质特异性受体的直接作用。低浓度胆碱可选择性增强醋酸酯引起的收缩，而乙酰胆碱、尼古丁、5 - 羟色胺和组胺引起的收缩则不受影响。然而，即使存在胆碱，N - 醋酸酯也不会引起收缩。有机磷胆碱酯酶抑制剂，如二异丙基氟磷酸酯和对氧磷，可选择性且不可逆地抑制阿司匹林和N,O - 二乙酰对氨基酚在有或无胆碱情况下的作用。从这些结果可以得出结论，有或无胆碱的醋酸酯通过胆碱能系统起作用。然而，它们的作用无法用已知机制来解释，如乙酰胆碱释放、胆碱酯酶抑制或直接的毒蕈碱样作用。因此，包括被认为是乙酰胆碱释放剂的苯醋酸酯在内的醋酸酯，似乎具有一种迄今未描述的胆碱能作用类型，其机制尚不清楚。制备物中的有机磷敏感酯酶似乎对于有或无胆碱的醋酸酯作用的起始至关重要，但胆碱作用的机制尚不清楚。
