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Potency of novel oximes to reactivate sarin inhibited human cholinesterases
D Jun, K Kuca, J Picha, V Koleckar, J Marek
Language English Country United States
NLK
Medline Complete (EBSCOhost)
from 2000-02-01 to 1 year ago
- MeSH
- Acetylcholinesterase metabolism MeSH
- Antidotes pharmacology MeSH
- Cholinesterase Inhibitors toxicity MeSH
- Financing, Organized MeSH
- Humans MeSH
- Molecular Structure MeSH
- Brain enzymology drug effects MeSH
- Obidoxime Chloride pharmacology MeSH
- Oximes pharmacology MeSH
- Pralidoxime Compounds pharmacology MeSH
- Pyridinium Compounds pharmacology MeSH
- Cholinesterase Reactivators pharmacology MeSH
- Sarin toxicity MeSH
- In Vitro Techniques MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
Class of monoquaternary pyridinium oximes was in vitro tested as potential reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) inhibited by nerve agent sarin. Human brain homogenate was used as an appropriate source of cholinesterases. Reactivation potency of novel oximes was compared with currently available reactivators - pralidoxime, obidoxime, and HI-6. According to the obtained results, only five reactivators were able to satisfactorily renew cholinesterase potency (pralidoxime, obidoxime, HI-6, 4-PAM, and K119). Unfortunately, none of the novel tested reactivators surpassed the reactivation potency of the currently most promising reactivator, HI-6. This study shows that monoquaternary reactivators are unable to reactivate nerve agent-inhibited AChE. Due to this, in future, only bisquaternary compounds derived from HI-6 or obidoxime should be designed as new potential cholinesterase reactivators.
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