目前用于对抗神经毒剂中毒的胆碱酯酶复活剂：它们在体外的有效性比较。

Currently used cholinesterase reactivators against nerve agent intoxication: comparison of their effectivity in vitro.

作者信息

Kuca Kamil, Jun Daniel, Bajgar Jiri

机构信息

Department of Toxicology, Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.

出版信息

Drug Chem Toxicol. 2007;30(1):31-40. doi: 10.1080/01480540601017637.

DOI:10.1080/01480540601017637

PMID:17364862

Abstract

In vitro comparison of reactivation efficacy of five currently used oximes - pralidoxime, obidoxime, trimedoxime, methoxime, and HI-6 (at two concentrations: 10-5 and 10-3 M) - against acetylcholinesterase (AChE; E.C. 3.1.1.7) inhibited by six different nerve agents (VX, Russian VX, sarin, cyclosarin, tabun, soman) and organophosphorus insecticide chlorpyrifos was the aim of this study. As a source of AChE in the experiments, rat brain homogenate was used. According to the results obtained, no AChE reactivator was able to reach sufficient potency for AChE inhibited by all nerve agents used. Moreover, oxime HI-6 (the most effective one) was not able to reactivate tabun- and soman-inhibited AChE. Due to this fact, it could be designated as a partially broad-spectrum reactivator.

摘要

本研究旨在对目前使用的五种肟类化合物——解磷定、双复磷、氯磷定、甲磺磷定和HI-6（两种浓度：10⁻⁵和10⁻³ M）——针对六种不同神经毒剂（VX、俄罗斯VX、沙林、环沙林、塔崩、梭曼）和有机磷杀虫剂毒死蜱抑制的乙酰胆碱酯酶（AChE；E.C. 3.1.1.7）进行体外再活化效果比较。实验中使用大鼠脑匀浆作为AChE的来源。根据所得结果，没有一种AChE复活剂能够对所有使用的神经毒剂抑制的AChE达到足够的效力。此外，肟类化合物HI-6（最有效的一种）无法使被塔崩和梭曼抑制的AChE再活化。鉴于此，它可被指定为一种部分广谱再活化剂。