Abstract
The efficacy of a bispyridinium oxime 1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide, called K033, and of currently used oximes (pralidoxime, obidoxime, oxime HI-6), to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun cyclosarin) was tested by in vitro methods. The new oxime K033 was found to be a more efficacious reactivator of sarin or cyclosarin-inhibited acetylcholinesterase than pralidoxime and obidoxime but it did not reach the efficacy of oxime HI-6 in the case of the inhibition of acetylcholinesterase by sarin or cyclosarin. On the other hand, oxime K033 was more efficacious than oxime HI-6 in reactivating tabun-inhibited acetylcholinesterase. Thus, oxime K033 seems to be a relatively efficacious broad spectrum acetylcholinesterase reactivator and, therefore, could be useful if no information about the type of nerve agent used was available.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / chemistry
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Acetylcholinesterase / metabolism*
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Animals
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Brain / drug effects
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Brain / enzymology
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Chemical Warfare Agents / pharmacology*
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Cholinesterase Inhibitors / pharmacology*
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Cholinesterase Reactivators / pharmacology*
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Male
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Obidoxime Chloride / pharmacology
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Organophosphates / pharmacology*
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Organophosphorus Compounds / pharmacology*
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Oximes / pharmacology*
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Pralidoxime Compounds / pharmacology
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Pyridinium Compounds / pharmacology*
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Rats
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Rats, Wistar
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Sarin / pharmacology*
Substances
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1,4-bis(2-hydroxyiminomethylpyridinium)butane
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Chemical Warfare Agents
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Cholinesterase Inhibitors
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Cholinesterase Reactivators
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Organophosphates
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Organophosphorus Compounds
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Oximes
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Pralidoxime Compounds
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Pyridinium Compounds
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Obidoxime Chloride
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Sarin
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Acetylcholinesterase
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asoxime chloride
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pralidoxime
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tabun
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cyclohexyl methylphosphonofluoridate