Most cited article - PubMed ID 19778210
A comparison of reactivating and therapeutic efficacy of newly-developed oximes (K156, K203) and commonly used oximes (obidoxime, HI-6) in cyclosarin-poisoned rats and mice
We have evaluated in vitro the potency of 23 oximes to reactivate human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) inhibited by racemic leptophos-oxon (O-[4-bromo-2,5-dichlorophenyl]-O-methyl phenyl-phosphonate), a toxic metabolite of the pesticide leptophos. Compounds were assayed in concentrations of 10 and 100 μM. In case of leptophos-oxon inhibited AChE, the best reactivation potency was achieved with methoxime, trimedoxime, obidoxime and oxime K027. The most potent reactivators of inhibited BChE were K033, obidoxime, K117, bis-3-PA, K075, K074 and K127. The reactivation efficacy of tested oximes was lower in case of leptophos-oxon inhibited BChE.
- Keywords
- acetylcholinesterase, butyrylcholinesterase, leptophos-oxon, nerve agent, oxime, pesticide, reactivator, scavenger,
- MeSH
- Acetylcholinesterase chemistry MeSH
- Butyrylcholinesterase chemistry MeSH
- Erythrocytes drug effects enzymology MeSH
- Leptophos analogs & derivatives chemistry pharmacology MeSH
- Humans MeSH
- Oximes chemistry MeSH
- Pesticides chemistry pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Butyrylcholinesterase MeSH
- Leptophos MeSH
- leptophos oxon MeSH Browser
- Oximes MeSH
- Pesticides MeSH