In vitro reactivation potency of acetylcholinesterase reactivators--K074 and K075--to reactivate tabun-inhibited human brain cholinesterases
Language English Country United States Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
17449453
DOI
10.1007/bf03033389
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase metabolism MeSH
- Enzyme Activation drug effects MeSH
- Butanes chemistry pharmacology MeSH
- Cholinesterase Inhibitors toxicity MeSH
- Humans MeSH
- Caudate Nucleus drug effects enzymology MeSH
- Obidoxime Chloride chemistry pharmacology MeSH
- Organophosphates toxicity MeSH
- Oximes chemistry pharmacology MeSH
- Pralidoxime Compounds chemistry pharmacology MeSH
- Pyridinium Compounds chemistry pharmacology MeSH
- Cholinesterase Reactivators chemistry pharmacology MeSH
- In Vitro Techniques MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide MeSH Browser
- Acetylcholinesterase MeSH
- asoxime chloride MeSH Browser
- Butanes MeSH
- Cholinesterase Inhibitors MeSH
- K075 compound MeSH Browser
- N,N'-monomethylenebis(pyridiniumaldoxime) MeSH Browser
- Obidoxime Chloride MeSH
- Organophosphates MeSH
- Oximes MeSH
- pralidoxime MeSH Browser
- Pralidoxime Compounds MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
- tabun MeSH Browser
In this work, two oximes for the treatment of tabun-inhibited acetylcholinesterase (AChE; EC 3.1.1.7), K074 (1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide) and K075 ((E)-1,4-bis(4-hydroxyiminomethylpyridinium)but-2-en dibromide), were tested in vitro as reactivators of AChE. Comparison was made with currently used AChE reactivators (pralidoxime, HI-6, methoxime and obidoxime). Human brain homogenate was taken as an appropriate source of the cholinesterases. As resulted, oxime K074 appears to be the most potent reactivator of tabun-inhibited AChE, with reactivation potency comparable to that of obidoxime. A second AChE reactivator, K075, does not attain as great a reactivation potency as K074, although its maximal reactivation (17%) was achieved at relevant concentrations for humans.
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