In vitro comparison of two most promising H-oximes (HI-6 and HLo-7) and currently commercially available reactivators pralidoxime and obidoxime in reactivation of cyclosarin-inhibited human cholinesterases

被引:1
|
作者
Kuca, Kamil [1 ]
Cabal, Jiri [1 ]
Jun, Daniel [1 ]
Koleckar, Vit [1 ]
机构
[1] Univ Def, Ctr Adv Studies, Fac Mil Hlth Sci, Dept Toxicol, Hradec Kralove 50001, Czech Republic
关键词
cholinesterase; reactivators; cyclosarin; nerve agent; oxime;
D O I
10.1080/15376510701380323
中图分类号
R99 [毒物学(毒理学)];
学科分类号
100405 ;
摘要
This study describes the evaluation of the in vitro ability of two acetylcholinesterase (EC 3.1.1.7) reactivators, HI-6 and HLo-7, very promising at present, to reactivate human brain cholinesterases inhibited by the nerve agent cyclosarin. The results obtained (percentage of reactivation and appropriate constants characterizing the whole reactivation process) were compared with two currently available reactivators on the market: pralidoxime and obidoxime. It is clear that both promising oximes surpassed the potency of standard reactivators, especially at human relevant concentrations (10(-4) M and lower). Because of the prohibition of such experiments on humans, data obtained in this study could be used as input data for prediction of in vivo action of these drugs in future.
引用
收藏
页码:329 / 333
页数:5
相关论文
共 3 条
  • [1] In vitro potency of H oximes (HI-6, HLo-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase
    Kuca, Kamil
    Cabal, Jiri
    Kassa, Jiri
    Jun, Daniel
    Hrabinova, Martina
    [J]. JOURNAL OF TOXICOLOGY AND ENVIRONMENTAL HEALTH-PART A-CURRENT ISSUES, 2006, 69 (15): : 1431 - 1440
  • [2] Commercially available antidotes of organophosphate poisonings (pralidoxime, obidoxime, methoxime, trimedoxime and HI-6) and newly developed oxime K027 as reactivators of human acetylcholinesterase inhibited by selected organophosphate pesticides
    Jun, Daniel
    Musilova, Lucie
    Kuca, Kamil
    Novotny, Ladislav
    [J]. TOXICOLOGY LETTERS, 2009, 189 : S217 - S217
  • [3] A comparison of the potency of newly developed oximes (K005, K027, K033, K048) and currently used oximes (pralidoxime, obidoxime, HI-6) to reactivate sarin-inhibited rat brain acetylcholinesterase by in vitro methods
    Kuca, K
    Cabal, J
    Kassa, J
    [J]. JOURNAL OF TOXICOLOGY AND ENVIRONMENTAL HEALTH-PART A-CURRENT ISSUES, 2005, 68 (08): : 677 - 686