A comparison of the potency of newly developed oximes (K005, K027, K033, K048) and currently used oximes (pralidoxime, obidoxime, HI-6) to reactivate sarin-inhibited rat brain acetylcholinesterase by in vitro methods
Language English Country Great Britain, England Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Acetylcholinesterase metabolism MeSH
- Chemical Warfare Agents toxicity MeSH
- Cholinesterase Inhibitors toxicity MeSH
- Rats MeSH
- Cells, Cultured MeSH
- Brain drug effects enzymology MeSH
- Oximes pharmacology MeSH
- Rats, Wistar MeSH
- Sarin antagonists & inhibitors toxicity MeSH
- Structure-Activity Relationship 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
- Acetylcholinesterase MeSH
- Chemical Warfare Agents MeSH
- Cholinesterase Inhibitors MeSH
- Oximes MeSH
- Sarin MeSH
The potency of newly developed and currently used oximes to reactivate sarin-inhibited acetylcholinesterase was evaluated using in vitro methods. A rat brain homogenate was used as a source of acetylcholinesterase. Significant differences in reactivation potency among all tested oximes were observed. Although the ability of newly developed oximes to reactivate sarin-inhibited acetylcholinesterase does not reach the reactivating potency of the oxime HI-6, the oxime K033 seems to be a more efficacious reactivator of sarin-inhibited acetylcholinesterase than other currently available oximes (pralidoxime, obidoxime) at concentrations (10(-5)-10(-4)M) corresponding to recommended doses in vivo. The results of our study also confirm that the reactivation potency of the tested reactivators depends on many factors, such as (1) the number of pyridinium rings, (2) the number of oxime groups and their position, and (3) the length and the shape of the linkage bridge between pyridinium rings.
References provided by Crossref.org
Experimental and Established Oximes as Pretreatment before Acute Exposure to Azinphos-Methyl
Combined Pre- and Posttreatment of Paraoxon Exposure
