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大鼠体内抗胆碱酯酶梭曼的持久性;与这种有机磷酸酯无毒模拟物的拮抗作用。

Persistence of the anti-cholinesterase soman in rats; antagonism with a non-toxic simulator of this organophosphate.

作者信息

Wolthuis O L, Benschop H P, Berends F

出版信息

Eur J Pharmacol. 1981 Jan 29;69(3):379-83. doi: 10.1016/0014-2999(81)90488-x.

Abstract

Anaesthetized, atropinized rats were poisoned with 6x LD50 soman (1,2,2,-trimethylpropyl methylphosphonofluoridate). Purified acetylcholinesterase, injected i.v. 75 min later, was rapidly inhibited, presumably by soman stored in a 'depot' from which it was gradually released. Existence of a depot is supported by the effect of a soman-simulator ('som-sim'), an organophosphonate structurally similar to soman but devoid of anti-cholinesterase activity. Som-sim can expel soman from the depot, or counteract its formation. Som-sim prophylaxis greatly enhances survival.

摘要

将大鼠麻醉并注射阿托品后,用6倍半数致死量的梭曼(1,2,2-三甲基丙基甲基膦酰氟)进行中毒处理。75分钟后静脉注射纯化的乙酰胆碱酯酶,该酶迅速受到抑制,推测是被储存在“储存库”中的梭曼抑制,梭曼从该“储存库”中逐渐释放。一种梭曼模拟物(“som-sim”)的作用支持了“储存库”的存在,“som-sim”是一种结构与梭曼相似但无抗胆碱酯酶活性的有机膦酸盐。“som-sim”可以将梭曼从“储存库”中排出,或抵消其形成。“som-sim”预防措施可大大提高存活率。

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