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
Language English Country England, Great Britain Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Drug Antagonism MeSH
- Diaphragm drug effects enzymology MeSH
- Cholinesterase Inhibitors toxicity MeSH
- Rats MeSH
- Lethal Dose 50 MeSH
- Brain drug effects enzymology MeSH
- Neurotoxicity Syndromes drug therapy prevention & control MeSH
- Oximes therapeutic use MeSH
- Rats, Wistar MeSH
- Pyridinium Compounds therapeutic use MeSH
- Cholinesterase Reactivators therapeutic use MeSH
- Sarin toxicity MeSH
- Dose-Response Relationship, Drug MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- BI 6 MeSH Browser
- Cholinesterase Inhibitors MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators 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.
References provided by Crossref.org
Reactivation of organophosphate-inhibited acetylcholinesterase by quaternary pyridinium aldoximes
