Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium--oximes
Language English Country England, Great Britain Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Acetylcholinesterase metabolism MeSH
- Cholinesterase Inhibitors chemistry pharmacology MeSH
- Kinetics MeSH
- Rats MeSH
- Brain drug effects enzymology MeSH
- Organophosphorus Compounds chemistry pharmacology MeSH
- Oximes chemistry pharmacology MeSH
- Pyridinium Compounds chemistry pharmacology MeSH
- Cholinesterase Reactivators chemistry pharmacology MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Cholinesterase Inhibitors MeSH
- cyclohexyl methylphosphonofluoridate MeSH Browser
- Organophosphorus Compounds MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators 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).
References provided by Crossref.org
Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes
The acute toxicity of acetylcholinesterase reactivators in mice in relation to their structure
