对塔崩抑制的乙酰胆碱酯酶有效的双季铵重活化剂。

Effective bisquaternary reactivators of tabun-inhibited AChE.

作者信息

Kuca Kamil, Cabal Jiri, Musilek Kamil, Jun Daniel, Bajgar Jiri

机构信息

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

出版信息

J Appl Toxicol. 2005 Nov-Dec;25(6):491-5. doi: 10.1002/jat.1084.

DOI:10.1002/jat.1084

PMID:16092078

Abstract

Two cholinesterase reactivators (K074 and K075) were synthesized and their reactivation efficacy against tabun-inhibited acetylcholinesterase of the rat brain was tested in vitro. Comparing this efficacy showed that commonly used oximes (pralidoxim, obidoxime and HI-6) were practically without reactivation potency. On the other hand, oximes K074, K075 and trimedoxime were satisfactorily effective. Moreover, K-oximes reactivated tabun-inhibited AChE at lower concentration (10(-4) and 10(-3) m) in comparison with trimedoxime (10(-3) and 10(-2) m). Thus, K-oximes can be considered as the most effective reactivators of tabun-inhibited AChE at present.

摘要

合成了两种胆碱酯酶复活剂（K074和K075），并在体外测试了它们对大鼠脑内塔崩抑制的乙酰胆碱酯酶的复活效果。比较这种效果表明，常用的肟类化合物（解磷定、双复磷和HI-6）实际上没有复活能力。另一方面，肟类化合物K074、K075和氯磷定效果令人满意。此外，与氯磷定（10(-3)和10(-2) m）相比，K-肟类化合物在较低浓度（10(-4)和10(-3) m）下就能复活塔崩抑制的乙酰胆碱酯酶。因此，K-肟类化合物目前可被认为是塔崩抑制的乙酰胆碱酯酶最有效的复活剂。