Department of Toxicology, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic.
Medicinal Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Yusong, Taejon 305-606, Korea.
Int J Mol Sci. 2008 Nov;9(11):2243-2252. doi: 10.3390/ijms9112243. Epub 2008 Nov 14.
The therapeutical efficacies of eleven oxime-based acetylcholinesterase reactivators were compared in an in vivo (rat model) study of treatment of intoxication caused by tabun. In this group there were some currently available oximes (obidoxime, trimedoxime and HI-6) and the rest were newly synthesized compounds. The best reactivation efficacy for acetylcholinesterase in blood (expressed as percent of reactivation) among the currently available oximes was observed after administration of trimedoxime (16%) and of the newly synthesized K127 (22432) (25%). The reactivation of butyrylcholinesterase in plasma was also studied; the best reactivators were trimedoxime, K117 (22435), and K127 (22432), with overall reactivation efficacies of approximately 30%. Partial protection of brain ChE against tabun inhibition was observed after administration of trimedoxime (acetylcholinesterase 20%; butyrylcholinesterase 30%) and obidoxime (acetylcholinesterase 12%; butyrylcholinesterase 16%).
在沙林中毒治疗的体内(大鼠模型)研究中,比较了 11 种基于肟的乙酰胆碱酯酶重激活剂的治疗效果。在这一组中,有一些现有的肟(双解磷、曲双解磷和 HI-6)和其余的是新合成的化合物。在现有的肟中,血液中乙酰胆碱酯酶的最佳重激活效果(以重激活的百分比表示)是曲双解磷(16%)和新合成的 K127(22432)(25%)。还研究了血浆中丁酰胆碱酯酶的重激活;最好的重激活剂是曲双解磷、K117(22435)和 K127(22432),总体重激活效率约为 30%。在给予曲双解磷(乙酰胆碱酯酶 20%;丁酰胆碱酯酶 30%)和双解磷(乙酰胆碱酯酶 12%;丁酰胆碱酯酶 16%)后,观察到对脑 ChE 对沙林抑制的部分保护。