Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium--oximes
Jazyk angličtina Země Anglie, Velká Británie Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- acetylcholinesterasa metabolismus MeSH
- cholinesterasové inhibitory chemie farmakologie MeSH
- kinetika MeSH
- krysa rodu Rattus MeSH
- mozek účinky léků enzymologie MeSH
- organofosforové sloučeniny chemie farmakologie MeSH
- oximy chemie farmakologie MeSH
- pyridinové sloučeniny chemie farmakologie MeSH
- reaktivátory cholinesterázy chemie farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- cholinesterasové inhibitory MeSH
- cyclohexyl methylphosphonofluoridate MeSH Prohlížeč
- organofosforové sloučeniny MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
Cyclohexyl methylphosphonofluoridate (cyclosarin, cyclosin, GF) is a highly toxic organophosphate, which is resistant to conventional oxime therapy. To gain insight into the reactivation kinetics, rat brain acetylcholinesterase (AChE) was inhibited in vitro by cyclosarin (pH 8.0, 25 degrees C) and reactivated with 22 different pyridiniumoximes. Three compounds were shown to be superior to the other oximes: 4-carbamoyl-4'-[(hydroxyimino)methyl]-1,1'-(oxydimethylene)dipyridin-1-ium dichloride (HS-6), 4'-carbamoyl-2-[(hydroxyimino)methyl]-1,1'-(oxydimethylene)dipyridin-1-ium dichloride (HI-6), and 4'-carbamoyl-2-[(hydroxyimino)-methyl]-1,1'-(but-2-ene-1,4-diyl)dipyridin-1-ium dichloride (BI-6).
Citace poskytuje Crossref.org
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