A comparison of the efficacy of a new asymmetric bispyridinium oxime BI-6 with presently used oximes and H oximes against sarin by in vitro and in vivo methods
Jazyk angličtina Země Anglie, Velká Británie Médium print
Typ dokumentu srovnávací studie, časopisecké články, práce podpořená grantem
- MeSH
- antagonismus léků MeSH
- bránice účinky léků enzymologie MeSH
- cholinesterasové inhibitory toxicita MeSH
- krysa rodu Rattus MeSH
- LD50 MeSH
- mozek účinky léků enzymologie MeSH
- neurotoxické syndromy farmakoterapie prevence a kontrola MeSH
- oximy terapeutické užití MeSH
- potkani Wistar MeSH
- pyridinové sloučeniny terapeutické užití MeSH
- reaktivátory cholinesterázy terapeutické užití MeSH
- sarin toxicita MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
- Názvy látek
- BI 6 MeSH Prohlížeč
- cholinesterasové inhibitory MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
- sarin MeSH
1. The reactivating and therapeutic efficacy of a new acetylcholinesterase reactivator, designated BI-6 (1-/2-hydroxyiminomethylpyridinium/-4-/carbamoylpyridinium/- 2-butene dibromide), against organophosphate sarin was compared with presently used oximes (pralidoxime, obidoxime, methoxime) and H oximes (HI-6, HLö-7) by in vitro and in vivo methods. 2. Our results confirm that the new oxime BI-6 is a significantly more efficacious acetylcholinesterase reactivator than currently available pralidoxime and obidoxime but not as effective as H oximes (HI-6, HLö-7) in vitro as well as in vivo. In addition, the oxime BI-6 is able to protect supralethal sarin poisoned rats at human-relevant doses. 3. Our data also suggest that the potency of oximes tested to reactivate sarin-inhibited acetylcholinesterase in vitro closely corresponds to their reactivating efficacy in vivo and their ability to protect rats poisoned with supralethal doses of sarin.
Citace poskytuje Crossref.org
Reactivation of organophosphate-inhibited acetylcholinesterase by quaternary pyridinium aldoximes
