使用肟类解毒剂使沙林抑制的猪脑乙酰胆碱酯酶重新激活。
Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes.
作者信息
Kuca Kamil, Jun Daniel
机构信息
Centre of Advanced Studies, Department of Toxicology, Faculty Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.
出版信息
J Med Toxicol. 2006 Dec;2(4):141-6. doi: 10.1007/BF03161181.
INTRODUCTION
Organophosphorus nerve agents inhibit the enzyme, acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators (also known as oximes) are generally used for the reactivation of an inhibited enzyme.
METHODS
Two new AChE reactivators--K033 and K027--were tested for their in vitro reactivation of sarin-inhibited pig-brain AChE. Their reactivation potencies were compared with the commercially available AChE reactivators, pralidoxime, obidoxime, and HI-6.
RESULTS
Of the oximes tested, the newly developed oxime K027 achieved the highest reactivation potency (100%; concentration of the oxime -10(-2) M). However, oxime HI-6 (33%) and obidoxime (23%) seem to be the best AChE reactivators for human relevant doses (10(-4) M and lower).
CONCLUSION
For human relevant doses, newly developed oximes (K027 and K033) do not surpass the reactivation potency of the most promising oxime, HI-6.
引言
有机磷神经毒剂会抑制乙酰胆碱酯酶（AChE；EC 3.1.1.7）。AChE重活化剂（也称为肟类化合物）通常用于使被抑制的酶重新活化。
方法
测试了两种新型AChE重活化剂——K033和K027——对沙林抑制的猪脑AChE的体外重活化作用。将它们的重活化效力与市售的AChE重活化剂解磷定、双复磷和HI-6进行比较。
结果
在所测试的肟类化合物中，新开发的肟类化合物K027具有最高的重活化效力（100%；肟类化合物浓度为10⁻² M）。然而，对于人体相关剂量（10⁻⁴ M及更低），肟类化合物HI-6（33%）和双复磷（23%）似乎是最佳的AChE重活化剂。
结论
对于人体相关剂量，新开发的肟类化合物（K027和K033）的重活化效力并未超过最有前景的肟类化合物HI-6。
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