Catecholamine 生合成に関する研究 (第4報) Thiourea 系化合物による Dopamine β-Hydroxylase 阻害作用

概要

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Some properties of dopamine β-hydroxylase (DβH) in the homogenate of bovine adrenal medulla and inhibitory effects of thiourea derivatives on DβH were examined. Enzymic formation of norsynephrine from tyramine in the homogenate of the adrenal medulla was linear with respect to time (up to 30 min) and protein concentration (up to 160 μg). By typical Lineweaver-Burk plots, Km value was calculated to be 4×10^<-3>M. Among the compounds tested, N-phenyl-N'-[3-(4H-1,2,4-triazolyl)]thiourea and N-n-butyl-N'-[3-(4H-1,2,4-triazolyl)]thiourea were effective inhibitors, and inhibition by the latter was non-competitive with substrate tyramine. Structure-activity relationship between thiourea derivatives and the inhibitory effect on DβH was discussed.
公益社団法人日本薬学会の論文
1975-04-25