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In vitro evaluation of acetylcholinesterase reactivators as potential antidotes against tabun nerve agent poisonings
- Source :
- Drug and chemical toxicology. 29(4)
- Publication Year :
- 2006
-
Abstract
- Searching for new potent acetylcholinesterase (AChE; E.C. 3.1.1.7) reactivators (oximes) is a very time-consuming process. At our department, we are able to synthesize more than 50 new AChE reactivators per year. Owing to this fact, we have to select promising reactivators using our in vitro method (potentiometric titration, pH 8 and temperature 25 degrees C; source of cholinesterases, rat brain homogenate; time of inhibition by nerve agents, 30 min; time of reactivation, 10 min) prior to in vivo experiments. For this purpose, we are using two-phase in vitro evaluation of reactivator potency. In the first phase, reactivation potency of all newly synthesized AChE reactivators is tested at two concentrations: 10(-3) M and 10(-5) M. Afterwards, all reactivators achieving reactivation potency over 15% (especially at the concentration 10(-5) M) are tested. The second phase consists of the measurement of the relationship between concentration of the oxime and its reactivation ability. In most cases, the reactivation bell-shaped curve is obtained. The most potent AChE reactivators are selected and provided for further experiments during our development process.
- Subjects :
- Cholinesterase Reactivators
Obidoxime Chloride
Health, Toxicology and Mutagenesis
Antidotes
Pharmacology
In Vitro Techniques
Toxicology
chemistry.chemical_compound
In vivo
medicine
Potency
Animals
Trimedoxime
Chemical Warfare Agents
Tabun
Nerve agent
Cholinesterase
Chemical Health and Safety
biology
Dose-Response Relationship, Drug
Molecular Structure
Chemistry
Public Health, Environmental and Occupational Health
Brain
General Medicine
Acetylcholinesterase
Organophosphates
Rats
Biochemistry
biology.protein
Cholinesterase Inhibitors
medicine.drug
Subjects
Details
- ISSN :
- 01480545
- Volume :
- 29
- Issue :
- 4
- Database :
- OpenAIRE
- Journal :
- Drug and chemical toxicology
- Accession number :
- edsair.doi.dedup.....5606717825e1cf3e1c0cc75369394956