Department of Toxicology, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic.
J Enzyme Inhib Med Chem. 2010 Aug;25(4):480-4. doi: 10.3109/14756360903257918.
The potency of newly developed bispyridinium compound K203 and its fluorinated analog KR-22836 in reactivating tabun-inhibited acetylcholinesterase and reducing tabun-induced lethal toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Studies determining the percentage of reactivation of tabun-inhibited blood and tissue acetylcholinesterase in rats showed that the reactivating efficacy of K203 is higher than the reactivating efficacy of its fluorinated analog KR-22836 as well as currently available oximes studied. The therapeutic efficacy of the oxime K203 and its fluorinated analog corresponds to their potency to reactivate tabun-inhibited acetylcholinesterase. According to the results, the oxime K203 is more suitable than KR-22836 for the replacement of commonly used oximes for the antidotal treatment of acute tabun poisoning due to its relatively high potency to counteract the acute toxicity of tabun.
新开发的双吡啶化合物 K203 及其氟化类似物 KR-22836 对塔崩抑制的乙酰胆碱酯酶的重活化作用及其降低塔崩诱导的致死毒性效应的效力与常用肟类化合物（解磷定、三甲肟、肟 HI-6）进行了比较，采用了体内方法。研究确定了 K203 在大鼠体内对塔崩抑制的血液和组织乙酰胆碱酯酶的再活化率，结果表明 K203 的再活化效力高于其氟化类似物 KR-22836 以及目前研究的可用肟类化合物。肟 K203 和其氟化类似物的治疗效果与其重活化塔崩抑制乙酰胆碱酯酶的效力相对应。根据结果，由于肟 K203 对塔崩的急性毒性具有相对较高的拮抗作用，因此比 KR-22836 更适合替代常用肟类化合物，用于急性塔崩中毒的解毒治疗。
