In vitro reactivation of acetylcholinesterase using the oxime K027
Language English Country United States Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
14748409
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase chemistry MeSH
- Cholinesterase Inhibitors MeSH
- Obidoxime Chloride chemistry MeSH
- Organophosphates MeSH
- Organothiophosphorus Compounds MeSH
- Oximes chemistry MeSH
- Pralidoxime Compounds chemistry MeSH
- Pyridinium Compounds chemistry MeSH
- Cholinesterase Reactivators chemistry MeSH
- Sarin MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide MeSH Browser
- Acetylcholinesterase MeSH
- asoxime chloride MeSH Browser
- Cholinesterase Inhibitors MeSH
- Obidoxime Chloride MeSH
- Organophosphates MeSH
- Organothiophosphorus Compounds MeSH
- Oximes MeSH
- pralidoxime MeSH Browser
- Pralidoxime Compounds MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
- Sarin MeSH
- tabun MeSH Browser
- VX MeSH Browser
The ability of a new bisquaternary oxime, K027 (1-[4-hydroxyiminomethylpyridinium]-3-[carbamoylpyridinium] propane dibromide), to reactivate the enzyme acetylcholinesterase (AChE) inhibited by the nerve agents Tabun, sarin and VX was evaluated. Its reactivation potency was compared to the AChE reactivators pralidoxime (2-PAM), obidoxime and HI-6; K027 seems a good reactivator of organophosphates-inhibited AChE. Its reactivation potency is lower compared to the other oximes for reactivation of sarin-inhibited AChE, but it is sufficient to significantly increase the activity of sarin-inhibited AChE. Its reactivation ability is comparable to obidoxime for reactivation of VX- and tabun-inhibited AChE and is higher than the reactivation potency of HI-6, for tabun-inhibited AChE. HI-6 is currently regarded the most promising reactivator of organophosphates-inhibited AChE.
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
Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes