Novel acetylcholinesterase reactivator--oxime K048--reactivation activity in vitro
Language English Country Netherlands Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
20402654
DOI
10.2174/157340610791208709
PII: MC-Abs-029a
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase metabolism MeSH
- Enzyme Activation drug effects MeSH
- Antidotes pharmacology MeSH
- Chemical Warfare Agents pharmacology MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Enzyme Reactivators pharmacology MeSH
- Rats MeSH
- Humans MeSH
- Organophosphorus Compounds pharmacology MeSH
- Oximes pharmacology MeSH
- Rats, Wistar MeSH
- Pyridinium Compounds pharmacology MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane MeSH Browser
- Acetylcholinesterase MeSH
- Antidotes MeSH
- Chemical Warfare Agents MeSH
- Cholinesterase Inhibitors MeSH
- Enzyme Reactivators MeSH
- Organophosphorus Compounds MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
A novel acetylcholinesterase (AChE) reactivator, a bispyridinium aldoxime named K048, was first synthesized in 2003. It is a promising antidote against tabun poisoning. Afterwards, other studies on several cholinesterases (ChE) of different species (humans, rats, etc.) and models (in vitro or in vivo) were conducted. We tested this oxime against nine different AChE inhibitors using in vitro tests on rat brain homogenate as source of enzyme. Our results showed that oxime K048 reached promising reactivation activity in case of all tested AChE inhibitors, except cyclosarin, at oxime concentration 10(-3) M. At a concentration of 10(-5) M, which is more common for human use, only methylchlorpyrifos-inhibited AChE was reactivated.
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