Literature DB >> 18547554

A comparison of reactivating efficacy of newly developed oximes (K074, K075) and currently available oximes (obidoxime, HI-6) in soman, cyclosarin and tabun-poisoned rats.

Jiri Kassa1, Daniel Jun, Jana Karasova, Jiri Bajgar, Kamil Kuca.   

Abstract

The potency of newly developed oximes (K074, K075) and commonly used oximes (obidoxime, HI-6) to reactivate nerve agent-inhibited acetylcholinesterase was evaluated in rats poisoned with soman, tabun or cyclosarin at a lethal dose corresponding to their LD(50) value. In vivo determined percentage of reactivation of soman-inhibited blood and brain acetylcholinesterase in poisoned rats showed that only the oxime HI-6 was able to reactivate soman-inhibited acetylcholinesterase in the peripheral (blood) as well as central (brain) compartment. In vivo determined percentage of reactivation of tabun-inhibited blood and brain acetylcholinesterase in poisoned rats showed that obidoxime is the most efficacious reactivator of tabun-inhibited acetylcholinesterase among studied oximes in the peripheral compartment (blood) while K074 seems to be the most efficacious reactivator of tabun-inhibited acetylcholinesterase among studied oximes in the central compartment (brain). In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among studied oximes. Due to their reactivating effects, both newly developed K oximes can be considered to be promising oximes for the antidotal treatment of acute tabun poisonings while the oxime HI-6 is still the most promising oxime for the treatment of acute soman and cyclosarin poisonings.

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Year:  2008        PMID: 18547554     DOI: 10.1016/j.cbi.2008.05.001

Source DB:  PubMed          Journal:  Chem Biol Interact        ISSN: 0009-2797            Impact factor:   5.192


  4 in total

1.  Molecular Modeling Studies on the Multistep Reactivation Process of Organophosphate-Inhibited Acetylcholinesterase and Butyrylcholinesterase.

Authors:  Jakub Jończyk; Jędrzej Kukułowicz; Kamil Łątka; Barbara Malawska; Young-Sik Jung; Kamil Musilek; Marek Bajda
Journal:  Biomolecules       Date:  2021-01-27

2.  Effect of several new and currently available oxime cholinesterase reactivators on tabun-intoxicated rats.

Authors:  Jana Zdarova Karasova; Jiri Kassa; Young-Sik Jung; Kamil Musilek; Miroslav Pohanka; Kamil Kuca
Journal:  Int J Mol Sci       Date:  2008-11-14       Impact factor: 6.208

3.  Effect of seven newly synthesized and currently available oxime cholinesterase reactivators on cyclosarin-intoxicated rats.

Authors:  Jana Zdarova Karasova; Jiri Kassa; Kamil Musilek; Miroslav Pohanka; Ladislav Novotny; Kamil Kuca
Journal:  Int J Mol Sci       Date:  2009-07-07       Impact factor: 6.208

4.  Advances in toxicology and medical treatment of chemical warfare nerve agents.

Authors:  Mohammd Moshiri; Emadodin Darchini-Maragheh; Mahdi Balali-Mood
Journal:  Daru       Date:  2012-11-28       Impact factor: 3.117

  4 in total

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