A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F18%3A50014332" target="_blank" >RIV/62690094:18470/18:50014332 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/18:10373438 RIV/60162694:G44__/18:43889531
Result on the web
<a href="https://bmcpharmacoltoxicol.biomedcentral.com/articles/10.1186/s40360-018-0196-3" target="_blank" >https://bmcpharmacoltoxicol.biomedcentral.com/articles/10.1186/s40360-018-0196-3</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1186/s40360-018-0196-3" target="_blank" >10.1186/s40360-018-0196-3</a>

Result language
angličtina
Original language name
A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase
Original language description
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.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30107 - Medicinal chemistry

Project
<a href="/en/project/GA15-16701S" target="_blank" >GA15-16701S: Concept of non-quaternary reactivators AChE as the antidotes of organophsophorus poisoning - a new hope or a blind way?</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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