A comparison of the ability of a new bispyridinium oxime--1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane dibromide and currently used oximes to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods
Language English Country England, Great Britain Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Acetylcholinesterase metabolism MeSH
- Enzyme Activation drug effects MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Rats MeSH
- Molecular Structure MeSH
- Brain enzymology MeSH
- Nervous System drug effects MeSH
- Oximes pharmacology MeSH
- Rats, Wistar MeSH
- Pyridinium Compounds pharmacology MeSH
- Cholinesterase Reactivators pharmacology MeSH
- In Vitro Techniques MeSH
- Dose-Response Relationship, Drug 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)-4-(4-carbamoylpyridinium)butane MeSH Browser
- Acetylcholinesterase MeSH
- Cholinesterase Inhibitors MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
The efficacy of a new bispyridinium oxime 1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane dibromide, called K048, and currently used oximes (pralidoxime, obidoxime, the oxime HI-6) to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun, cyclosarin, VX) was tested by in vitro methods. The new oxime K048 was found to be a more efficacious reactivator of nerve agent-inhibited acetylcholinesterase than pralidoxime (in the case of VX, tabun and cyclosarin), obidoxime (cyclosarin and tabun) and HI-6 (tabun) but it did not reach the efficacy of currently used oximes for the reactivation of acetylcholinesterase inhibited by sarin. Thus, the oxime K048 seems to be a relatively efficacious broad spectrum acetylcholinesterase reactivator and, therefore, it could be useful for the treatment of a nerve agent-exposed population if information about detection of the type of nerve agent is not available.
References provided by Crossref.org
Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016-2019)
Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study
Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes
Reactivation of organophosphate-inhibited acetylcholinesterase by quaternary pyridinium aldoximes
