Antidotal efficacy of pyridinium oximes and cholineacetyltransferase inhibitors against organophosphorus intoxication in rodents.
In an attempt to develop effective antidote against organophosphorus intoxication, some new imidazole-pyridinium mono-oximes, long chain pyridinium mono-oximes and cholineacetyltransferase inhibitors were synthesised. These compounds were evaluated for their in vivo therapeutic protection and neuromuscular function studies in rodents. The results indicate that SPK-series oximes may be useful against sarin poisoning without any beneficial effect against VX (O-Ethyl S-2-NN-diisopropylaminoethyl methylphosphonofluoridate) intoxication. The cholineacetyltransferase (ChAT) inhibitors may not be of any help against any of the OP compounds studied in this study.
Dube
S N
SN
Defence Research and Development Establishment, Gwalior.
Kumar
D
D
Acharya
J
J
Dubey
D K
DK
Purnanand
Sikder
A K
AK
D000818:Animals; D000931:Antidotes / Q000138:chemical synthesis / Q000494:pharmacology*; D002795:Choline O-Acetyltransferase / Q000037:antagonists & inhibitors*; D002800:Cholinesterase Inhibitors / Q000633:toxicity*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009469:Neuromuscular Junction / Q000187:drug effects; D009943:Organophosphorus Compounds / Q000037:antagonists & inhibitors* / Q000633:toxicity*; D009946:Organothiophosphorus Compounds / Q000633:toxicity; D010091:Oximes / Q000138:chemical synthesis / Q000494:pharmacology*; D011726:Pyridinium Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012524:Sarin / Q000633:toxicity
D000931:Antidotes; D002795:Choline O-Acetyltransferase; D002800:Cholinesterase Inhibitors; D004791:Enzyme Inhibitors; D009943:Organophosphorus Compounds; D009946:Organothiophosphorus Compounds; D010091:Oximes; D011726:Pyridinium Compounds; D012524:Sarin; C104222:SPK 3; C009680:VX-agent