A comparison of the efficacy of a bispyridinium oxime--1,4-bis-(2-hydroxyiminomethylpyridinium) butane dibromide and currently used oximes to reactivate sarin, tabun or cyclosarin-inhibited acetylcholinesterase by in vitro methods.
The efficacy of a bispyridinium oxime 1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide, called K033, and of currently used oximes (pralidoxime, obidoxime, oxime HI-6), to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun cyclosarin) was tested by in vitro methods. The new oxime K033 was found to be a more efficacious reactivator of sarin or cyclosarin-inhibited acetylcholinesterase than pralidoxime and obidoxime but it did not reach the efficacy of oxime HI-6 in the case of the inhibition of acetylcholinesterase by sarin or cyclosarin. On the other hand, oxime K033 was more efficacious than oxime HI-6 in reactivating tabun-inhibited acetylcholinesterase. Thus, oxime K033 seems to be a relatively efficacious broad spectrum acetylcholinesterase reactivator and, therefore, could be useful if no information about the type of nerve agent used was available.
Kuca
K
K
Purkynĕ Military Medical Academy, Department of Toxicology, Hradec Králové, Czech Republic. kucakam@pmfhk.cz
Cabal
J
J
Kassa
J
J
D000110:Acetylcholinesterase / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology; 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*; D009943:Organophosphorus Compounds / Q000494:pharmacology*; D010091:Oximes / Q000494:pharmacology*; D011220:Pralidoxime Compounds / Q000494:pharmacology; D011726:Pyridinium Compounds / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012524:Sarin / Q000494:pharmacology*
C489959:1,4-bis(2-hydroxyiminomethylpyridinium)butane; D002619:Chemical Warfare Agents; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D010755:Organophosphates; D009943:Organophosphorus Compounds; D010091:Oximes; D011220:Pralidoxime Compounds; D011726:Pyridinium Compounds; D009768:Obidoxime Chloride; D012524:Sarin; D000110:Acetylcholinesterase; C022870:asoxime chloride; C028797:pralidoxime; C009374:tabun; C053914:cyclohexyl methylphosphonofluoridate