The Effect of Neutral Oximes on the Reactivation of Human Acetylcholinesterase Inhibited with Paraoxon

被引：31
|
作者：
Ribeiro, Tatiana S. [1 ]
Prates, Arthur [2 ]
Alves, Sergio R. [2 ]
Oliveira-Silva, Jefferson J. [2 ]
Riehl, Carlos A. S. [3 ]
Daniel Figueroa-Villar, J. [1 ]
机构：
[1] Inst Mil Engn, Dept Quim, BR-22290270 Rio De Janeiro, RJ, Brazil
[2] Fiocruz MS, ENSP, CESTEH, BR-21041210 Rio De Janeiro, RJ, Brazil
[3] Univ Fed Rio de Janeiro, Inst Quim, Ilha Fundao, Rio De Janeiro, RJ, Brazil
来源：
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY | 2012年 / 23卷 / 07期
关键词：
neutral oximes; huAChE reactivation; paraoxon; chemical warfare; (thiophen-2-yl)aldoxime; CHEMICAL WARFARE AGENTS; ORGANOPHOSPHORUS COMPOUNDS; BISQUATERNARY OXIMES; MOLECULAR-DYNAMICS; PYRIDINIUM OXIMES; KINETIC-ANALYSIS; IN-VITRO; TABUN; SARIN; BUTYRYLCHOLINESTERASE;
D O I：
10.1590/S0103-50532012000700004
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Important defense agents against chemical warfare weapons, which are reactivators of human acetylcholinesterase (huAChE) inhibited by neurotoxic organophosphorus compounds (OP), need a reasonable permeation of the hematoencephalic barrier (HB). In this work, neutral oximes, which permeate HB better than the cationic oximes currently used as defense agents, were tested as reactivators of huAChE inhibited with paraoxon using the modified Ellman test with pralidoxime (2-PAM) as positive standard. The most active neutral oxime was (thiophen-2-yl) aldoxime, which reactivated 93% of the inhibited huAChE and was 12% more effective than 2-PAM. The results showed that simple neutral oximes have potential to function as antidotes for intoxication with neurotoxic OPs, suggesting further research on the development of neutral defense agents.
引用
收藏
页码：1216 / +
页数：27
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