双季铵肟作为塔崩抑制的人脑海胆碱酯酶的重活化剂：一项体外研究。

Bisquaternary oximes as reactivators of tabun-inhibited human brain cholinesterases: an in vitro study.

作者信息

Kuca Kamil, Jun Daniel, Cabal Jiri, Musilova Lucie

机构信息

Center of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.

出版信息

Basic Clin Pharmacol Toxicol. 2007 Jul;101(1):25-8. doi: 10.1111/j.1742-7843.2007.00085.x.

DOI:10.1111/j.1742-7843.2007.00085.x

PMID:17577312

Abstract

Intoxications caused by tabun nerve agent are generally very hard to treat by convential acetylcholinesterase (AChE) reactivators. Due to this, new AChE reactivators are still developed. In this study, we have tested three new promising bisquaternary AChE reactivators: K027, K033 and K048. These reactivators were previously tested on rat brain homogenate. To mimic reality, we studied the potency of these new oximes to reactivate tabun-inhibited human brain cholinesterases. As is evident from the results, reactivator K048 (reactivation 40%) surpassed all reactivators tested in this study [including the most promising ones, namely trimedoxime (37%) and obidoxime (33%)]. Moreover, if compared to our previous results from rat brain studies, species differences were demonstrated.

摘要

由塔崩神经毒剂引起的中毒通常很难用传统的乙酰胆碱酯酶（AChE）复活剂进行治疗。因此，新型AChE复活剂仍在不断研发。在本研究中，我们测试了三种有前景的新型双季铵AChE复活剂：K027、K033和K048。这些复活剂之前已在大鼠脑匀浆上进行过测试。为模拟实际情况，我们研究了这些新型肟类化合物对被塔崩抑制的人脑海胆碱酯酶的复活能力。从结果中可以明显看出，复活剂K048（复活率40%）超过了本研究中测试的所有复活剂[包括最有前景的三甲肟（37%）和双复磷（33%）]。此外，与我们之前在大鼠脑研究中的结果相比，显示出了种属差异。