A comparison of reactivating and therapeutic efficacy of the oxime K203 and its fluorinated analog (KR-22836) with currently available oximes (obidoxime, trimedoxime, HI-6) against tabun in rats and mice
Language English Country Great Britain, England Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Antidotes pharmacology therapeutic use MeSH
- Cholinesterase Inhibitors toxicity MeSH
- Rats MeSH
- Mice MeSH
- Obidoxime Chloride pharmacology therapeutic use MeSH
- Organophosphates toxicity MeSH
- Oximes pharmacology therapeutic use MeSH
- Pyridinium Compounds pharmacology therapeutic use MeSH
- Cholinesterase Reactivators pharmacology therapeutic use MeSH
- Trimedoxime pharmacology therapeutic use MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- 1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene MeSH Browser
- Antidotes MeSH
- asoxime chloride MeSH Browser
- Cholinesterase Inhibitors MeSH
- Obidoxime Chloride MeSH
- Organophosphates MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
- tabun MeSH Browser
- Trimedoxime MeSH
The potency of newly developed bispyridinium compound K203 and its fluorinated analog KR-22836 in reactivating tabun-inhibited acetylcholinesterase and reducing tabun-induced lethal toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Studies determining the percentage of reactivation of tabun-inhibited blood and tissue acetylcholinesterase in rats showed that the reactivating efficacy of K203 is higher than the reactivating efficacy of its fluorinated analog KR-22836 as well as currently available oximes studied. The therapeutic efficacy of the oxime K203 and its fluorinated analog corresponds to their potency to reactivate tabun-inhibited acetylcholinesterase. According to the results, the oxime K203 is more suitable than KR-22836 for the replacement of commonly used oximes for the antidotal treatment of acute tabun poisoning due to its relatively high potency to counteract the acute toxicity of tabun.
References provided by Crossref.org
Strategies for enhanced bioavailability of oxime reactivators in the central nervous system
Time-dependent changes of oxime K027 concentrations in different parts of rat central nervous system
