In vitro potency of H oximes (HI-6, HLö-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase.
The efficacy of H oximes (HI-6, HLö-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate acetylcholinesterase inhibited by two nerve agents (tabun, VX agent) was tested in vitro. Both H oximes (HI-6, HLö-7) and the oxime BI-6 were found to be more efficacious reactivators of VX-inhibited acetylcholinesterase than pralidoxime and obidoxime. On the other hand, their potency to reactivate tabun-inhibited acetylcholinesterase was low and did not reach the reactivating efficacy of trimedoxime and obidoxime. Thus, none of these compounds can be considered to be a broad-spectrum reactivator of nerve agent-inhibited acetylcholinesterase in spite of high potency to reactivate acetylcholinesterase inhibited by some nerve agents. More than one oxime may be necessary for the antidotal treatment of nerve agent-exposed individuals.
Kuca
Kamil
K
Department of Toxicology, Faculty of Military Health Sciences, Hradec Králové, Czech Republic.
Cabal
Jiri
J
Kassa
Jiri
J
Jun
Daniel
D
Hrabinova
Martina
M
D000110:Acetylcholinesterase / Q000502:physiology*; D000818:Animals; D000931:Antidotes / Q000494:pharmacology; D001921:Brain / Q000187:drug effects*; D002619:Chemical Warfare Agents / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology; D002801:Cholinesterase Reactivators / Q000494:pharmacology*; D008297:Male; D009768:Obidoxime Chloride / Q000494:pharmacology; D010755:Organophosphates / Q000494:pharmacology; D009946:Organothiophosphorus Compounds / Q000494:pharmacology; D010091:Oximes / Q000494:pharmacology*; D011220:Pralidoxime Compounds / Q000494:pharmacology; D011725:Pyridines / Q000494:pharmacology; D011726:Pyridinium Compounds / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D014289:Trimedoxime / Q000494:pharmacology
D000110:Acetylcholinesterase; D000931:Antidotes; D002619:Chemical Warfare Agents; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D009768:Obidoxime Chloride; D010755:Organophosphates; D009946:Organothiophosphorus Compounds; D010091:Oximes; D011220:Pralidoxime Compounds; D011725:Pyridines; D011726:Pyridinium Compounds; D014289:Trimedoxime; C118647:BI 6; C058577:HLo 7; C009680:VX-agent; C022870:asoxime chloride; C028797:pralidoxime; C009374:tabun