Effective bisquaternary reactivators of tabun-inhibited AChE
Language English Country England, Great Britain Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
PubMed
16092078
DOI
10.1002/jat.1084
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase chemistry metabolism MeSH
- Butanes chemistry pharmacology MeSH
- Cholinesterase Inhibitors toxicity MeSH
- Kinetics MeSH
- Rats MeSH
- Brain drug effects enzymology MeSH
- Organophosphates toxicity MeSH
- Oximes chemical synthesis pharmacology MeSH
- Rats, Wistar MeSH
- Pyridinium Compounds MeSH
- Pyrimidines chemistry pharmacology MeSH
- Cholinesterase Reactivators chemical synthesis pharmacology MeSH
- In Vitro Techniques MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Female 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(4-hydroxyiminomethylpyridinium)butane dibromide MeSH Browser
- Acetylcholinesterase MeSH
- Butanes MeSH
- Cholinesterase Inhibitors MeSH
- Organophosphates MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Pyrimidines MeSH
- Cholinesterase Reactivators MeSH
- tabun MeSH Browser
Two cholinesterase reactivators (K074 and K075) were synthesized and their reactivation efficacy against tabun-inhibited acetylcholinesterase of the rat brain was tested in vitro. Comparing this efficacy showed that commonly used oximes (pralidoxim, obidoxime and HI-6) were practically without reactivation potency. On the other hand, oximes K074, K075 and trimedoxime were satisfactorily effective. Moreover, K-oximes reactivated tabun-inhibited AChE at lower concentration (10(-4) and 10(-3) m) in comparison with trimedoxime (10(-3) and 10(-2) m). Thus, K-oximes can be considered as the most effective reactivators of tabun-inhibited AChE at present.
References provided by Crossref.org
Acute Toxic Injuries of Rat's Visceral Tissues Induced by Different Oximes
Toxic Injury to Muscle Tissue of Rats Following Acute Oximes Exposure
Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study