In vitro reactivation of sarin-inhibited brain acetylcholinesterase from different species by various oximes
Language English Country Great Britain, England Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Acetylcholinesterase metabolism MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Species Specificity MeSH
- Kinetics MeSH
- Rats MeSH
- Humans MeSH
- Brain drug effects enzymology MeSH
- Obidoxime Chloride metabolism pharmacology MeSH
- Oximes metabolism pharmacology MeSH
- Pralidoxime Compounds metabolism pharmacology MeSH
- Swine MeSH
- Pyridinium Compounds metabolism pharmacology MeSH
- Cholinesterase Reactivators pharmacology MeSH
- Sarin pharmacology MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- 1,4-bis(2-hydroxyiminomethylpyridinium)butane MeSH Browser
- Acetylcholinesterase MeSH
- asoxime chloride MeSH Browser
- Cholinesterase Inhibitors MeSH
- Obidoxime Chloride MeSH
- Oximes MeSH
- pralidoxime MeSH Browser
- Pralidoxime Compounds MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
- Sarin MeSH
In vitro as well as in vivo evaluation of the reactivating efficacy of various oximes against nerve agent-inhibited acetylcholinesterase has been usually done with the help of animal experiments. Nevertheless, previously published data indicate that the reactivation potency of oximes may be different in human and animal species, which may hamper the extrapolation of animal data to human data. Therefore, to better evaluate the efficacy of various oximes (pralidoxime, obidoxime, HI-6, K033) to reactivate brain acetylcholinesterase inhibited by sarin by in vitro methods, human, rat and pig brain acetylcholinesterase were used to calculate kinetic parameters for the reactivation. Our results show differences among the species, depending on the type of oxime, and indicate that data from animal experiments needs to be carefully evaluated before extrapolation to humans.
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