Glickman_1984_Toxicol.Appl.Pharmacol_73_16

Reference

Title : Profenofos insecticide bioactivation in relation to antidote action and the stereospecificity of acetylcholinesterase inhibition, reactivation, and aging - Glickman_1984_Toxicol.Appl.Pharmacol_73_16
Author(s) : Glickman AH , Wing KD , Casida JE
Ref : Toxicology & Applied Pharmacology , 73 :16 , 1984
Abstract :

Poisoning signs in chicks administered the organophosphorus insecticide profenofos correlated with in vivo inhibition of brain acetylcholinesterase (AChE) activity. Mixtures of atropine with eserine, pyridinium oximes, or the bispyridinium compound SAD-128 increased the LD50 of coadministered profenofos by up to sevenfold in chicks and fourfold in mice. Atropine and the oximes were less effective as profenofos antidotes, indicating that profenofos-inhibited AChE may undergo rapid aging. Brain AChE from chicks poisoned with profenofos was not reactivated by pralidoxime methanesulfonate, although it was from chicks poisoned with the phosphoramidothiolate, methamidophos. Similarly, eel AChE, inhibited in vitro by bioactivated (-)-profenofos, the most toxic isomer, did not reactivate in contrast to that inhibited by methamidophos, nonbioactivated (-)-profenofos, and (+)-profenofos, with or without bioactivation. It appears that the action of eserine and possibly SAD-128 was due to protecting AChE or cholinergic receptors from profenofos or bioactivated profenofos and that oximes may work in the same way rather than as reactivators due to rapid aging of the inhibited AChE.

PubMedSearch : Glickman_1984_Toxicol.Appl.Pharmacol_73_16
PubMedID: 6710513

Related information

Inhibitor Profenofos
Reactivator Profenofos    SAD-128    P2s~contrathion

Citations formats

Glickman AH, Wing KD, Casida JE (1984)
Profenofos insecticide bioactivation in relation to antidote action and the stereospecificity of acetylcholinesterase inhibition, reactivation, and aging
Toxicology & Applied Pharmacology 73 :16

Glickman AH, Wing KD, Casida JE (1984)
Toxicology & Applied Pharmacology 73 :16