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[丙泮尼地作为拮抗剂:神经肌肉接头乙酰胆碱酯酶的竞争性抑制剂]

[Propanidid as an antagonist: competitive inhibitor of neuromuscular plaque acetylcholinesterase].

作者信息

Pesando O T, Piazza L, Berruti G, Sciandra G

出版信息

Minerva Anestesiol. 1980 Jun;46(6):665-70.

PMID:7465080
Abstract

Propanidid is a competitive inhibitor not only of serum cholinesterase, but of neuromuscular plaque and brain acetylcholinesterase also. The I50 of plaque acetylcholinesterase occurs at much higher concentrations of anaesthetic than for serum enzyme, this may depend on the environmental conditions under which propanidide has to act, or on acetylcholinesterase's high degree of specificity by comparison with pseudocholinesterase. Succinylcholine also inhibits serum cholinesterase but not plaque enzyme. With respect to the serum enzyme, the inhibition curve of the two drugs combined is similar to that of propanidide alone. The prolongation of apnoea observed during propanidide-induced anaesthesia, when succinylcholine is administered, does not appear to be due to diminution of serum cholinesterase activity but rather to interference of the two other drugs with neuromuscular transmission.

摘要

丙泮尼地不仅是血清胆碱酯酶的竞争性抑制剂,也是神经肌肉斑块和脑乙酰胆碱酯酶的竞争性抑制剂。斑块乙酰胆碱酯酶的半数抑制浓度(I50)出现在比血清酶更高的麻醉剂浓度下,这可能取决于丙泮尼地发挥作用的环境条件,或者取决于与假性胆碱酯酶相比乙酰胆碱酯酶的高度特异性。琥珀酰胆碱也抑制血清胆碱酯酶,但不抑制斑块酶。就血清酶而言,两种药物联合使用的抑制曲线与单独使用丙泮尼地的抑制曲线相似。在丙泮尼地诱导的麻醉期间给予琥珀酰胆碱时观察到的呼吸暂停延长,似乎不是由于血清胆碱酯酶活性降低,而是由于其他两种药物对神经肌肉传递的干扰。

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