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H肟类化合物(HI-6、HLö-7)、肟类化合物BI-6以及目前使用的肟类化合物(解磷定、双复磷、三甲肟)对重新激活被神经毒剂抑制的大鼠脑乙酰胆碱酯酶的体外效力。

In vitro potency of H oximes (HI-6, HLö-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase.

作者信息

Kuca Kamil, Cabal Jiri, Kassa Jiri, Jun Daniel, Hrabinova Martina

机构信息

Department of Toxicology, Faculty of Military Health Sciences, Hradec Králové, Czech Republic.

出版信息

J Toxicol Environ Health A. 2006 Aug;69(15):1431-40. doi: 10.1080/15287390500364283.

DOI:10.1080/15287390500364283
PMID:16766478
Abstract

The efficacy of H oximes (HI-6, HLö-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate acetylcholinesterase inhibited by two nerve agents (tabun, VX agent) was tested in vitro. Both H oximes (HI-6, HLö-7) and the oxime BI-6 were found to be more efficacious reactivators of VX-inhibited acetylcholinesterase than pralidoxime and obidoxime. On the other hand, their potency to reactivate tabun-inhibited acetylcholinesterase was low and did not reach the reactivating efficacy of trimedoxime and obidoxime. Thus, none of these compounds can be considered to be a broad-spectrum reactivator of nerve agent-inhibited acetylcholinesterase in spite of high potency to reactivate acetylcholinesterase inhibited by some nerve agents. More than one oxime may be necessary for the antidotal treatment of nerve agent-exposed individuals.

摘要

在体外测试了H类肟(HI-6、HLö-7)、肟BI-6以及目前使用的肟(解磷定、双复磷、氯磷定)对两种神经毒剂(塔崩、VX毒剂)抑制的乙酰胆碱酯酶的重活化效果。发现H类肟(HI-6、HLö-7)和肟BI-6对VX抑制的乙酰胆碱酯酶的重活化效果比解磷定和双复磷更好。另一方面,它们对塔崩抑制的乙酰胆碱酯酶的重活化能力较低,未达到氯磷定和双复磷的重活化效果。因此,尽管这些化合物对某些神经毒剂抑制的乙酰胆碱酯酶有高效的重活化能力,但没有一种可被视为神经毒剂抑制的乙酰胆碱酯酶的广谱重活化剂。对于接触神经毒剂的个体进行解毒治疗可能需要不止一种肟。

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