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metadata.artigo.dc.title: A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase
metadata.artigo.dc.creator: Kuca, Kamil
Musilek, Kamil
Jun, Daniel
Zdarova-Karasova, Jana
Nepovimova, Eugenie
Soukup, Ondrej
Hrabinova, Martina
Mikler, John
Franca, Tanos C. C.
Cunha, Elaine F. F. da
Castro, Alexandre A. de
Valis, Martin
Ramalho, Teodorico C.
metadata.artigo.dc.subject: Chemical warfare agents
Acetylcholinesterase reactivator
Tabun exposure
Agentes de guerra química
Reativador de acetilcolinesterase
Exposição ao tabun
metadata.artigo.dc.publisher: BMC 2018
metadata.artigo.dc.identifier.citation: KUCA, K. et al. A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase. BMC Pharmacology and Toxicology, [S. l.], v. 19, n. 8, p. 1-10, 2018.
metadata.artigo.dc.description.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 (kr) of 2142 min− 1. M− 1, which was 51 times higher than that obtained for obidoxime (kr = 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.
metadata.artigo.dc.language: en_US
Appears in Collections:DQI - Artigos publicados em periódicos

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