A comparison of the efficacy of new asymmetric bispyridinium oximes (K027, K048) with currently available oximes against tabun by in vivo methods
Language English Country Great Britain, England Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
PubMed
16952906
DOI
10.1080/15287390600631730
PII: R507361N7V7HR152
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase metabolism MeSH
- Enzyme Activation MeSH
- Diaphragm enzymology MeSH
- Chemical Warfare Agents poisoning MeSH
- Rats MeSH
- Brain enzymology MeSH
- Organophosphates MeSH
- Organophosphate Poisoning * MeSH
- Poisoning drug therapy MeSH
- Oximes pharmacology MeSH
- Rats, Wistar MeSH
- Pyridinium Compounds pharmacology MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- 1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide MeSH Browser
- 1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane MeSH Browser
- Acetylcholinesterase MeSH
- Chemical Warfare Agents MeSH
- Organophosphates MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- tabun MeSH Browser
The potency of newly developed asymmetric bispyridinium oximes (K027, K048) in reactivating tabun-inhibited acetylcholinesterase (AChE) and in eliminating tabun-induced acute toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Studies determined the percent of reactivation of tabun-inhibited blood and tissue AChE in poisoned rats and showed that the reactivating efficacy of both newly developed oximes is comparable with obidoxime and trimedoxime, the most efficacious known reactivators of tabun-inhibited AChE. These were also found to be sufficiently efficacious in the elimination of acute lethal toxic effects in tabun-poisoned rats. The oxime HI-6, relatively efficacious against soman, did not seem to be an adequately effective oxime in reactivation of tabun-inhibited AChE and in counteracting acute lethal effects of tabun. In addition, our results confirm that the efficacy of oximes in reactivating tabun-inhibited AChE in blood, diaphragm, and brain correlates with the potency of oximes in protecting rats poisoned with supralethal doses of tabun.
References provided by Crossref.org
Experimental and Established Oximes as Pretreatment before Acute Exposure to Azinphos-Methyl
Combined Pre- and Posttreatment of Paraoxon Exposure
Two step synthesis of a non-symmetric acetylcholinesterase reactivator