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

被引:51
作者
Kuca, K [1 ]
Cabal, J [1 ]
机构
[1] Fac Mil Med Acad, Dept Toxicol, Hradec Kralove 50001, Czech Republic
关键词
acetylcholinesterase; HI-6; inhibition; organophosphates; oximes; reactivation; sarin; screening method;
D O I
10.1080/15376520590968770
中图分类号
R99 [毒物学(毒理学)];
学科分类号
100405 ;
摘要
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.
引用
收藏
页码:247 / 252
页数:6
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