Abstract
The dose-response relationships of phenethylamine derivatives and pentylamine as substrate or inhibitor of rat liver monoamine oxidase were investigated. Increased concentration of tyramine increased the rate of oxidative deamination which later decreased. This bell-shaped dose-response curve of tyramine agreed fairly well with the theoretical curve calculated from eq. (3). Dissociation constants of tyramine-monoamine oxidase complex were estimated to be Km=4.5×10-4M as a substrate and KI'=1.0×10-2M as an inhibitor. Phenethylamine, 4-methoxyphenethylamine, and pentylamine were more or less active as substrates of monoamine oxidase, but also inhibited monoamine oxidase at higher concentration partially non-competitively. From these results, it is concluded that these amines act both as a substrate and an inhibitor, and the dose-response curves of these amines can be represented by eq. (3).
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Schedule a callMore From: Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
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