Kassa Jiri, Kuca Kamil, Cabal Jiri, Paar Martin
Department of Toxicology, Faculty of Military Health Sciences, Hradec Králové, Czech Republic.
J Toxicol Environ Health A. 2006 Oct;69(20):1875-82. doi: 10.1080/15287390600631730.
The potency of newly developed asymmetric bispyridinium oximes (K027, K048) in reactivating tabun-inhibited acetylcholinesterase (AChE) and in eliminating tabun-induced acute toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Studies determined the percent of reactivation of tabun-inhibited blood and tissue AChE in poisoned rats and showed that the reactivating efficacy of both newly developed oximes is comparable with obidoxime and trimedoxime, the most efficacious known reactivators of tabun-inhibited AChE. These were also found to be sufficiently efficacious in the elimination of acute lethal toxic effects in tabun-poisoned rats. The oxime HI-6, relatively efficacious against soman, did not seem to be an adequately effective oxime in reactivation of tabun-inhibited AChE and in counteracting acute lethal effects of tabun. In addition, our results confirm that the efficacy of oximes in reactivating tabun-inhibited AChE in blood, diaphragm, and brain correlates with the potency of oximes in protecting rats poisoned with supralethal doses of tabun.
采用体内实验方法,将新开发的不对称双吡啶肟(K027、K048)与常用肟类(双复磷、双解磷、肟HI-6)在重新激活塔崩抑制的乙酰胆碱酯酶(AChE)以及消除塔崩诱导的急性毒性作用方面的效力进行了比较。研究测定了中毒大鼠体内塔崩抑制的血液和组织AChE的重新激活百分比,结果表明,两种新开发的肟类的重新激活效力与双复磷和双解磷相当,双复磷和双解磷是已知对塔崩抑制的AChE最有效的重新激活剂。还发现它们在消除塔崩中毒大鼠的急性致死毒性作用方面也足够有效。肟HI-6对梭曼相对有效,但在重新激活塔崩抑制的AChE以及对抗塔崩的急性致死作用方面似乎不是一种足够有效的肟类。此外,我们的结果证实,肟类在重新激活血液、膈肌和大脑中塔崩抑制的AChE方面的效力与肟类在保护超致死剂量塔崩中毒大鼠方面的效力相关。