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肟类化合物 K027:一种新型低毒化合物,可作为神经毒剂和农药抑制的乙酰胆碱酯酶的通用重活化剂。

Oxime K027: novel low-toxic candidate for the universal reactivator of nerve agent- and pesticide-inhibited acetylcholinesterase.

机构信息

Center of Advanced Studies, Faculty of Military Health Sciences, University of Defense, Trebesska, Hradec Kralove, Czech Republic.

出版信息

J Enzyme Inhib Med Chem. 2010 Aug;25(4):509-12. doi: 10.3109/14756360903357569.

Abstract

Oxime K027 is a low-toxic bisquaternary compound originally developed as a reactivator of acetylcholinesterase (AChE) inhibited by nerve agents. The reactivation potency of K027 has been tested as a potential reactivator of AChE inhibited by tabun, sarin, cyclosarin, soman, VX, Russian VX, paraoxon, methylchlorpyrifos, and DDVP. The results show that oxime K027 reactivated AChE inhibited by almost all tested inhibitors to more than 10%, which is believed to be enough for saving the lives of intoxicated organisms. In the case of cyclosarin- and soman-inhibited AChE, oxime K027 did not reach sufficient reactivation potency.

摘要

肟 K027 是一种低毒的双季铵化合物,最初是作为神经毒剂抑制的乙酰胆碱酯酶 (AChE) 的重活化剂开发的。K027 的重活化能力已被测试为一种潜在的 AChE 重活化剂,可对抗塔崩、沙林、梭曼、索曼、VX、俄罗斯 VX、对氧磷、甲基氯化吡啶和 DDVP 抑制。结果表明,肟 K027 使几乎所有测试抑制剂抑制的 AChE 重新活化超过 10%,这被认为足以拯救中毒生物的生命。在梭曼和索曼抑制的 AChE 的情况下,肟 K027 没有达到足够的重活化能力。

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