A comparison of reactivating and therapeutic efficacy of the oxime K203 and its fluorinated analog (KR-22836) with currently available oximes (obidoxime, trimedoxime, HI-6) against tabun in rats and mice
Jazyk angličtina Země Velká Británie, Anglie Médium print
Typ dokumentu srovnávací studie, časopisecké články, práce podpořená grantem
- MeSH
- antidota farmakologie terapeutické užití MeSH
- cholinesterasové inhibitory toxicita MeSH
- krysa rodu Rattus MeSH
- myši MeSH
- obidoxim chlorid farmakologie terapeutické užití MeSH
- organofosfáty toxicita MeSH
- oximy farmakologie terapeutické užití MeSH
- pyridinové sloučeniny farmakologie terapeutické užití MeSH
- reaktivátory cholinesterasy farmakologie terapeutické užití MeSH
- trimedoxim farmakologie terapeutické užití MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
- Názvy látek
- 1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene MeSH Prohlížeč
- antidota MeSH
- asoxime chloride MeSH Prohlížeč
- cholinesterasové inhibitory MeSH
- obidoxim chlorid MeSH
- organofosfáty MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterasy MeSH
- tabun MeSH Prohlížeč
- trimedoxim MeSH
The potency of newly developed bispyridinium compound K203 and its fluorinated analog KR-22836 in reactivating tabun-inhibited acetylcholinesterase and reducing tabun-induced lethal toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Studies determining the percentage of reactivation of tabun-inhibited blood and tissue acetylcholinesterase in rats showed that the reactivating efficacy of K203 is higher than the reactivating efficacy of its fluorinated analog KR-22836 as well as currently available oximes studied. The therapeutic efficacy of the oxime K203 and its fluorinated analog corresponds to their potency to reactivate tabun-inhibited acetylcholinesterase. According to the results, the oxime K203 is more suitable than KR-22836 for the replacement of commonly used oximes for the antidotal treatment of acute tabun poisoning due to its relatively high potency to counteract the acute toxicity of tabun.
Citace poskytuje Crossref.org
Strategies for enhanced bioavailability of oxime reactivators in the central nervous system
Time-dependent changes of oxime K027 concentrations in different parts of rat central nervous system
