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A comparison of the reactivating and therapeutic efficacy of two novel bispyridinium oximes (K305, K307) with the oxime K203 and trimedoxime in tabun-poisoned rats and mice
Jiri Kassa, Vendula Sepsova, Anna Horova, Kamil Musilek
Language English Country Czech Republic
Document type Research Support, Non-U.S. Gov't
- MeSH
- Acetylcholinesterase drug effects MeSH
- Antidotes administration & dosage pharmacology toxicity MeSH
- Atropine administration & dosage pharmacology toxicity MeSH
- Diaphragm enzymology MeSH
- Models, Animal MeSH
- Brain enzymology drug effects MeSH
- Mice, Mutant Strains MeSH
- Nerve Agents pharmacology chemistry toxicity MeSH
- Organophosphates pharmacology toxicity MeSH
- Oximes * pharmacology chemistry classification MeSH
- Rats, Wistar MeSH
- Cholinesterase Reactivators administration & dosage pharmacology toxicity MeSH
- Trimedoxime pharmacology chemistry classification MeSH
- Animals MeSH
- Check Tag
- Male MeSH
- Animals MeSH
- Publication type
- Research Support, Non-U.S. Gov't MeSH
The reactivating and therapeutic efficacy of two newly developed oximes (K305, K307) was compared with the oxime K203 and trimedoxime using in vivo methods The study determining percentage of reactivation of tabun-inhibited acetylcholinesterase in the peripheral as well as central nervous system (diaphragm, brain) in tabun-poisoned rats showed that the reactivating efficacy of both newly developed oximes is lower compared to the reactivating efficacy of the oxime K203 and trimedoxime. The therapeutic efficacy of all oximes studied roughly corresponds to their reactivating efficacy. While the ability of the oxime K305 to reduce acute toxicity of tabun in mice is approaching to the therapeutic efficacy of trimedoxime, the ability of another novel bispyridinium oxime K307 to reduce acute toxicity of tabun is significantly lower compared to trimedoxime and the oxime K203. Thus, the reactivating and therapeutic efficacy of both examined 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.
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Literatura
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- $a The reactivating and therapeutic efficacy of two newly developed oximes (K305, K307) was compared with the oxime K203 and trimedoxime using in vivo methods The study determining percentage of reactivation of tabun-inhibited acetylcholinesterase in the peripheral as well as central nervous system (diaphragm, brain) in tabun-poisoned rats showed that the reactivating efficacy of both newly developed oximes is lower compared to the reactivating efficacy of the oxime K203 and trimedoxime. The therapeutic efficacy of all oximes studied roughly corresponds to their reactivating efficacy. While the ability of the oxime K305 to reduce acute toxicity of tabun in mice is approaching to the therapeutic efficacy of trimedoxime, the ability of another novel bispyridinium oxime K307 to reduce acute toxicity of tabun is significantly lower compared to trimedoxime and the oxime K203. Thus, the reactivating and therapeutic efficacy of both examined 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.
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