Potency of novel oximes to reactivate sarin inhibited human cholinesterases

被引：9

作者：

Jun, Daniel ^{[1
,2
]}

Kuca, Kamil ^{[1
,2
]}

Picha, Jan ^{[3
]}

Koleckar, Vit ^{[2
]}

Marek, Jan ^{[4
]}

机构：

[1] Uni Def, Fac Mil Hlth Sci, Dept Toxicol, Trebesska 1575, Hradec Kralove 50001, Czech Republic

[2] Fac Mil Hlth Sci, Ctr Adv Studies, Hradec Kralove, Czech Republic

[3] Prague Inst Chem Technol, Dept Organ Chem, CR-16628 Prague, Czech Republic

[4] Charles Univ Prague, Fac Pharm Hradec Kralove, Hradec Kralove, Czech Republic

来源：

DRUG AND CHEMICAL TOXICOLOGY | 2008年 / 31卷 / 01期

关键词：

cholinesterase; sarin; nerve agent; reactivation; antidote;

D O I：

10.1080/01480540701688238

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Class of monoquaternary pyridinium oximes was in vitro tested as potential reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) inhibited by nerve agent sarin. Human brain homogenate was used as an appropriate source of cholinesterases. Reactivation potency of novel oximes was compared with currently available reactivators - pralidoxime, obidoxime, and HI-6. According to the obtained results, only five reactivators were able to satisfactorily renew cholinesterase potency (pralidoxime, obidoxime, HI-6, 4-PAM, and K119). Unfortunately, none of the novel tested reactivators surpassed the reactivation potency of the currently most promising reactivator, HI-6. This study shows that monoquaternary reactivators are unable to reactivate nerve agent-inhibited AChE. Due to this, in future, only bisquaternary compounds derived from HI-6 or obidoxime should be designed as new potential cholinesterase reactivators.

引用

页码：1 / 9

页数：9

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