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- W2015374299 abstract "The efficacy of the pesticide chlordimeform or N′-(4-chloro-o-tolyl)-N,N′-dimethylform-amidine, six chlordimeform metabolites, and eleven related compounds as inhibitors of the oxidative deamination of radiocarbon-labelled biogenic amines by rat brain monoamine oxidase was examined. The I50 value for chlordimeform with tyramine as substrate was 6.0 × 10−5M. Inhibition following prolonged pre-incubation of chlordimeform with monoamine oxidase increased with time. and this was attributed, at least in part, to the formation of the more potent monoamine oxidase inhibitor 4′-chloro-o-formotoluidide, a known chlordimeform metabolite and degradation product. 4′-Chloro-o-formotoluidide was the most potent monoamine oxidase inhibitor examined yielding I50 values of 2.6 × 10−6m. 1.5 × 10−6M and 3.2 × 10−6M, with tyramine, dopamine, and serotonin, respectively, as substrates. The N-demethyl (demethylchlordimeform) and N-didemethyl chlordimeform metabolites gave I50 values with tyramine of 3.3 × 10−5M and 7.5 × 10−5M, respectively. Three additional metabolites, 4-chloro-o-toluidine, 5-chloroanthranilic acid, and N-formyl-5-chloroanthranilic acid, were weak inhibitors with I50 values of 1 × 10−4m or higher. The other formamidine compounds also inhibited the oxidative deamination of tyramine; I50 values ranged from 9.3 × 10−5m to 7.5 × 10−6m. Lineweaver-Burk plots revealed that chlordimeform, demethylchlordimeform, and 4′-chloro-o-formotoluidide were competitive inhibitors of the oxidative deamination of β-phenylethylamine, tyramine, dopamine, tryptamine, and serotonin. Inhibition was reversible since activity was restored by washing." @default.
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- W2015374299 title "Inhibition of rat brain monoamine oxidase by formamidines and related compounds" @default.
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- W2015374299 doi "https://doi.org/10.1016/0028-3908(76)90086-1" @default.
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