In vitro reactivation of trichlorfon-inhibited butyrylcholinesterase using HI-6, obidoxime, pralidoxime and K048
Jazyk angličtina Země Velká Británie, Anglie Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
18825528
DOI
10.1080/14756360802328315
PII: 903104614
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa metabolismus MeSH
- Alzheimerova nemoc farmakoterapie enzymologie patologie MeSH
- butyrylcholinesterasa metabolismus MeSH
- cholinesterasové inhibitory chemie farmakologie terapeutické užití MeSH
- lidé MeSH
- obidoxim chlorid farmakologie MeSH
- oximy farmakologie MeSH
- pralidoximové sloučeniny farmakologie MeSH
- pyridinové sloučeniny farmakologie MeSH
- reaktivátory cholinesterasy chemie farmakologie terapeutické užití MeSH
- trichlorfon chemie farmakologie terapeutické užití MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane MeSH Prohlížeč
- acetylcholinesterasa MeSH
- asoxime chloride MeSH Prohlížeč
- butyrylcholinesterasa MeSH
- cholinesterasové inhibitory MeSH
- obidoxim chlorid MeSH
- oximy MeSH
- pralidoxime MeSH Prohlížeč
- pralidoximové sloučeniny MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterasy MeSH
- trichlorfon MeSH
Trichlorfon is a specific inhibitor of cholinesterases. It was typically used as an insecticide; however, trichlorfon was described as useful for symptomatic treatment of Alzheimer's disease some years ago. The presented study is aimed at reactivation of trichlorfon-inhibited butyrylcholinesterase since this enzyme play an important role in Alzheimer's disease as deputy for acetylcholinesterase and furthermore it could be applied as a scavenger in case of overdosing. We used in vitro reactivation test for considering only reactivation efficacy of butyrylcholinesterase that is inhibited by trichlorfon and not reactivation of butyrylcholinesterase inhibited by trichlorfon metabolic products. Four reactivators were used: HI-6, pralidoxime, obidoxime, and K048. Although all of the reactivators seem to be effective at 1 mM concentration, a lower concentration was not able ensure sufficient reactivation. There was also an observed lowering of reactivation efficacy when butyrylcholinesterase was exposed to trichlorfon for a longer time interval.
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