新型沙林神经毒剂抑制脑乙酰胆碱酯酶重激活剂的评价。

Evaluation of newly synthesized reactivators of the brain cholinesterase inhibited by sarin nerve agent.

机构信息

Department of Toxicology, Faculty of Military Medical Academy, Trebesska 1575, Hradec KralovéCzech Republic.

出版信息

Toxicol Mech Methods. 2005;15(4):247-52. doi: 10.1080/15376520590968770.

DOI:10.1080/15376520590968770

PMID:20021089

Abstract

In this work in vitro evaluation of the reactivation potency of the newly synthesized reactivators for acetylcholinesterase (AChE; EC 3.1.1.7) is described. Using this method, reactivation potency of 21 potential reactivators of AChE inhibited by the nerve agent sarin has been evaluated. We have confirmed the fact that currently the most promising AChE reactivator, HI-6, is the most effective reactivator of sarin-inhibited AChE. There are only three AChE reactivators-HI-6, TO033 and TO047-able to satisfactorily reactivate sarin-inhibited AChE at the concentration 10(-5) M, which is nontoxic for human use. On the other hand, there are 14 AChE reactivators, that are able to reactivate sarin-inhibited AChE at the concentration 10(-3) M. However, this concentration of reactivator is probably toxic for human use.

摘要

本工作对新合成的乙酰胆碱酯酶（AChE；EC 3.1.1.7）重激活剂的体外活性进行了评估。使用该方法，评估了 21 种可能的沙林抑制的 AChE 重激活剂的重激活活性。我们已经证实，目前最有前途的 AChE 重激活剂 HI-6 是沙林抑制的 AChE 最有效的重激活剂。只有三种 AChE 重激活剂——HI-6、TO033 和 TO047——能够在 10^-5 M 的浓度下令人满意地重激活沙林抑制的 AChE，而该浓度对人体使用是无毒的。另一方面，有 14 种 AChE 重激活剂能够在 10^-3 M 的浓度下重激活沙林抑制的 AChE。然而，这种重激活剂的浓度对人体使用可能是有毒的。