Nejvíce citovaný článek - PubMed ID 17674811
A comparison of reactivating efficacy of newly developed oximes (K074, K075) and currently available oximes (obidoxime, HI-6) in cyclosarin-and tabun-poisoned rats
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.
- Klíčová slova
- Antidotes, Chemical warfare agents, Oxime, Poisoning, Reactivator, Treatment,
- MeSH
- acetylcholinesterasa metabolismus MeSH
- antidota metabolismus MeSH
- cholinesterasové inhibitory metabolismus MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- mozek enzymologie MeSH
- organofosfáty metabolismus MeSH
- oximy metabolismus MeSH
- pyridinové sloučeniny metabolismus MeSH
- reaktivátory cholinesterasy metabolismus MeSH
- simulace molekulového dockingu MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene MeSH Prohlížeč
- acetylcholinesterasa MeSH
- antidota MeSH
- cholinesterasové inhibitory MeSH
- organofosfáty MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterasy MeSH
- tabun MeSH Prohlížeč
