Kuca K, Cabal J, Kassa J
Purkynĕ Military Medical Academy, Department of Toxicology, Hradec Králové, Czech Republic.
Pharmazie. 2004 Oct;59(10):795-8.
The efficacy of a bispyridinium oxime 1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide, called K033, and of currently used oximes (pralidoxime, obidoxime, oxime HI-6), to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun cyclosarin) was tested by in vitro methods. The new oxime K033 was found to be a more efficacious reactivator of sarin or cyclosarin-inhibited acetylcholinesterase than pralidoxime and obidoxime but it did not reach the efficacy of oxime HI-6 in the case of the inhibition of acetylcholinesterase by sarin or cyclosarin. On the other hand, oxime K033 was more efficacious than oxime HI-6 in reactivating tabun-inhibited acetylcholinesterase. Thus, oxime K033 seems to be a relatively efficacious broad spectrum acetylcholinesterase reactivator and, therefore, could be useful if no information about the type of nerve agent used was available.
通过体外方法测试了一种双吡啶肟1,4-双(2-羟基亚氨基甲基吡啶鎓)丁烷二溴化物(称为K033)以及目前使用的肟类药物(解磷定、双复磷、肟HI-6)对各种神经毒剂(沙林、塔崩、环沙林)抑制的乙酰胆碱酯酶的重新激活效果。发现新型肟K033在重新激活沙林或环沙林抑制的乙酰胆碱酯酶方面比解磷定和双复磷更有效,但在沙林或环沙林抑制乙酰胆碱酯酶的情况下,其效果未达到肟HI-6的水平。另一方面,在重新激活塔崩抑制的乙酰胆碱酯酶方面,肟K033比肟HI-6更有效。因此,肟K033似乎是一种相对有效的广谱乙酰胆碱酯酶重新激活剂,所以在无法获得所使用神经毒剂类型信息的情况下可能会很有用。