A comparison of the reactivating and therapeutic efficacy of two novel bispyridinium oximes (K920, K923) with the oxime K203 and trimedoxime in tabun-poisoned rats and mice

被引:1
|
作者
Kassa, Jiri [1 ]
Sepsova, Vendula [1 ]
Horova, Anna [1 ]
Musilek, Kamil [1 ]
机构
[1] Fac Mil Hlth Sci, Dept Toxicol & Mil Pharm, Hradec Kralove 50001, Czech Republic
关键词
Tabun; Acetylcholinesterase; Oximes; Rats; Mice; CHEMICAL WARFARE AGENTS; BRAIN-BARRIER PENETRATION; COMMONLY USED OXIMES; INHIBITED ACETYLCHOLINESTERASE; ORGANOPHOSPHORUS COMPOUNDS; PYRIDINIUM-OXIMES; IN-VITRO; PESTICIDES; ANTIDOTES; OBIDOXIME;
D O I
10.1016/j.jab.2015.07.002
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
The potency of two novel oximes (K920, K923) to reactivate tabun-inhibited acetylcholinesterase and to reduce acute toxicity of tabun was compared with the oxime K203 and trimedoxime using in vivo methods. The study determining percentage of reactivation of tabun-inhibited peripheral acetylcholinesterase (diaphragm) and central acetylcholinesterase (brain) in tabun-poisoned rats showed that the reactivating efficacy of both newly developed oximes is lower than the reactivating potency of the oxime K203 and trimedoxime. The therapeutic efficacy of both newly developed oximes roughly corresponds to their weak reactivating efficacy. Their potency to reduce acute toxicity of tabun in mice was lower compared to the oxime K203 and trimedoxime. All differences in reactivating efficacy of oximes and different protective ratios were found for selected doses of oximes used in this study. Based on the results obtained, we can conclude that the reactivating and therapeutic potency of both newly developed oximes does not prevail the effectiveness of the oxime K203 and trimedoxime and, therefore, they are not suitable for their replacement of commonly used oximes for the treatment of acute tabun poisoning. The conclusion is only relevant for the experimental animals used in this study because of remarkable species differences in reactivating properties of oximes. (C) 2015 Faculty of Health and Social Studies, University of South Bohemia in Ceske Budejovice. Published by Elsevier Sp. z o.o. All rights reserved.
引用
收藏
页码:299 / 304
页数:6
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  • [31] A comparison of the reactivating and therapeutic efficacy of newly developed oximes (K347, K628) with commonly used oximes (obidoxime, HI-6) against tabun in rats and mice
    Kassa, Jiri
    Karasova, Jana Zdarova
    Kuca, Kamil
    Musilek, Kamil
    [J]. DRUG AND CHEMICAL TOXICOLOGY, 2010, 33 (03) : 227 - 232
  • [32] A comparison of the neuroprotective efficacy of individual oxime (HI-6) and combinations of oximes (HI-6+trimedoxime, HI-6+K203) in soman-poisoned rats
    Kassa, Jiri
    Karasova, Jana Zdarova
    Tesarova, Sandra
    [J]. DRUG AND CHEMICAL TOXICOLOGY, 2011, 34 (03) : 233 - 239
  • [33] Efficacy of two new asymmetric bispyridinium oximes (K-27 and K-48) in rats exposed to diisopropylfluorophosphate: comparison with pralidoxime, obidoxime, trimedoxime, methoxime, and HI-6
    Lorke, D. E.
    Hasan, M. Y.
    Nurulain, S. M.
    Kuca, K.
    Schmitt, A.
    Petroianu, G. A.
    [J]. TOXICOLOGY MECHANISMS AND METHODS, 2009, 19 (04) : 327 - 333
  • [34] Efficacy of two new asymmetric bispyridinium oximes (K-27 and K-48) in rats exposed to diisopropylfluorophosphate (DFP): Comparison with the established oximes pralidoxime, obidoxime, trimedoxime, methoxime and HI-6
    Hasan, M. Y.
    Lorke, D. E.
    Nurulain, S. M.
    Kuca, K.
    Schmitt, A.
    Petmianu, G. A.
    [J]. CLINICAL TOXICOLOGY, 2008, 46 (05) : 397 - 398
  • [35] Comments on "Efficacy of two new asymmetric bispyridinium oximes (K-27 and K-48) in rats exposed to diisopropylfluorophosphate: Comparison with pralidoxime, obidoxime, trimedoxime, methoxime, and HI 6"
    Theirmann, Horst
    Worek, Franz
    Eyer, Peter
    [J]. TOXICOLOGY MECHANISMS AND METHODS, 2009, 19 (04): : 334 - 334
  • [36] An evaluation of reactivating and therapeutic efficacy of newly developed oximes (K206, K269) and commonly used oximes (obidoxime, HI-6) in cyclosarin-poisoned rats and mice
    Kassa, Jiri
    Karasova, Jana
    Musilek, Kamil
    Kuca, Kamil
    Bajgar, Jiri
    [J]. CLINICAL TOXICOLOGY, 2009, 47 (01) : 72 - 76
  • [37] Comments on "Efficacy of two new asymmetric bispyridinium oximes (K-27 and K-48) in rats exposed to diisopropylfluorophosphate: Comparison with pralidoxime, obidoxime, trimedoxime, methoxime, and HI 6" Response
    Lorke, Dietrich E.
    Petroianu, Georg A.
    [J]. TOXICOLOGY MECHANISMS AND METHODS, 2009, 19 (04): : 335 - 335