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A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase
- Source :
- BMC Pharmacology and Toxicology, Vol 19, Iss 1, Pp 1-10 (2018), BMC Pharmacology & Toxicology
- Publication Year :
- 2018
- Publisher :
- BMC, 2018.
-
Abstract
- Background Based on in vitro and in vivo rat experiments, the newly developed acetylcholinesterase (AChE) reactivator, K203, appears to be much more effective in the treatment of tabun poisonings than currently fielded oximes. Methods To determine if this reactivating efficacy would extend to humans, studies were conducted in vitro using human brain homogenate as the source of AChE. The efficacy of K203 was compared with commercially available oximes; pralidoxime, obidoxime and asoxime (HI-6). Results Reactivation studies showed that K203 was the most effective reactivator with a second order kinetic constant (k r) of 2142 min− 1. M− 1, which was 51 times higher than that obtained for obidoxime (k r = 42 min− 1. M− 1). Both pralidoxime and asoxime (HI-6) failed to significantly reactivate tabun-inhibited human AChE. Discussion According to these results and previous studies, using K203, it appears that oxime K203 is the most effective reactivator of tabun-inhibited cholinesterase in several species including humans and should be considered as a possible medical countermeasure to tabun exposure.
- Subjects :
- 0301 basic medicine
Obidoxime
Cholinesterase Reactivators
Pralidoxime
Aché
Antidotes
Chemical warfare agents
Pyridinium Compounds
Pharmacology
01 natural sciences
Oxime
03 medical and health sciences
chemistry.chemical_compound
In vivo
lcsh:RA1190-1270
Oximes
medicine
Animals
Humans
Pharmacology (medical)
Cholinesterase
Tabun
lcsh:Toxicology. Poisons
biology
Poisoning
010401 analytical chemistry
Reactivator
lcsh:RM1-950
Brain
Acetylcholinesterase
language.human_language
Organophosphates
0104 chemical sciences
Rats
Molecular Docking Simulation
Treatment
030104 developmental biology
lcsh:Therapeutics. Pharmacology
chemistry
biology.protein
language
Cholinesterase Inhibitors
medicine.drug
Research Article
Subjects
Details
- Language :
- English
- ISSN :
- 20506511
- Volume :
- 19
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- BMC Pharmacology and Toxicology
- Accession number :
- edsair.doi.dedup.....c3a8ac53305d7d2ee2c9627be5873401