Novel acetylcholinesterase reactivator--oxime K048--reactivation activity in vitro
Jazyk angličtina Země Nizozemsko Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
20402654
DOI
10.2174/157340610791208709
PII: MC-Abs-029a
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa metabolismus MeSH
- aktivace enzymů účinky léků MeSH
- antidota farmakologie MeSH
- chemické bojové látky farmakologie MeSH
- cholinesterasové inhibitory farmakologie MeSH
- enzymové reaktivátory farmakologie MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- organofosforové sloučeniny farmakologie MeSH
- oximy farmakologie MeSH
- potkani Wistar MeSH
- pyridinové sloučeniny farmakologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane MeSH Prohlížeč
- acetylcholinesterasa MeSH
- antidota MeSH
- chemické bojové látky MeSH
- cholinesterasové inhibitory MeSH
- enzymové reaktivátory MeSH
- organofosforové sloučeniny MeSH
- oximy MeSH
- pyridinové sloučeniny 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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