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Hasegawa L, Imamura T: Inhibitory effect of various organophosphorus esters on rat liver malathion carboxylesterase in vitro: role of mixed-function oxidases. Toxicol Lett. 1985 Aug;26(2-3):225-31. 6 Structurally related trialkyl phosphorothioates were assessed for their inhibitory effects on rat liver malathion carboxylesterase in vitro. IC50 values indicate that all these compounds, except compound III, a phosphorodithioate, inhibited the activity of the enzyme progressively with increasing incubation time of the compounds with the enzyme preparation. Compounds with an ethyl substitution were more potent than the corresponding methyl-substituted inhibitors. There was cytochrome P-450-mediated oxidative deactivation of all compounds tested, this was especially profound with inhibitors containing an ethyl thiolate moiety. |
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