Moritoki H, Shinohara Y, Yamauchi M, Ishida Y
Eur J Pharmacol. 1978 Jan 1;47(1):95-102. doi: 10.1016/0014-2999(78)90379-5.
Acetate esters, such as phenyl acetate and aspirin, induced atropine-sensitive contractions of isolated uterus only when choline was present. These contractions were selectively and reversibly inhibited by carbamate-type cholinesterase inhibitors, such as neostigmine and eserine, and quaternary ammonium compounds, such as tetraethylammonium and decamethonium. After treatment with organophosphorus cholinesterase inhibitors, such as di-isopropyl fluorophosphate and tetraethyl pyrophosphate, the uterus failed to respond to the acetate esters, even when high concentrations of choline were present. The inhibition of the response of the uterus by organophosphates was effectively removed by pyridine-2-aldoxime methiodide. Pretreatment of the uterus with neostigmine or simultaneous addition of high concentrations of quaternary ammonium compounds prevented the inhibition by organophosphates. The inhibition produced by neostigmine was also reduced by simultaneous addition of quaternary ammonium compounds. These findings suggest that some esterase having an anionic site and an esteratic site, probably cholinesterase, may mediate in the uterine contractions induced by acetate esters in the presence of choline, and that inhibition by organophosphates, carbamates and quaternary ammonium compounds of cholinesterase activity in the preparation may impede the initiation of contractions by the acetate esters in the presence of choline.
只有在胆碱存在时，醋酸酯（如苯乙酸酯和阿司匹林）才会引起离体子宫的阿托品敏感收缩。这些收缩可被氨基甲酸酯类胆碱酯酶抑制剂（如新斯的明和毒扁豆碱）以及季铵化合物（如四乙铵和十烃季铵）选择性且可逆地抑制。在用有机磷胆碱酯酶抑制剂（如二异丙基氟磷酸酯和焦磷酸四乙酯）处理后，即使存在高浓度的胆碱，子宫也不再对醋酸酯产生反应。吡啶 - 2 - 醛肟甲碘化物可有效消除有机磷对子宫反应的抑制作用。用新斯的明预处理子宫或同时添加高浓度的季铵化合物可防止有机磷的抑制作用。同时添加季铵化合物也可降低新斯的明产生的抑制作用。这些发现表明，某种具有阴离子位点和酯解位点的酯酶（可能是胆碱酯酶）可能在胆碱存在时介导醋酸酯诱导的子宫收缩，并且制剂中有机磷、氨基甲酸酯和季铵化合物对胆碱酯酶活性的抑制可能会阻碍胆碱存在时醋酸酯引发的收缩。
