モノアミン酸化酵素阻害剤の研究(第2報) : Phenethylamine誘導体の作用

概要

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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 K_m=4.5×10^<-4>M as a substrate and K_I'=1.0×10^<-2>M 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).
公益社団法人日本薬学会の論文
1966-06-25