Xenobiotica 1975-02-01

Inhibitors of hepatic mixed function oxidases. I. The metabolism of 2,6-dihydroxy-,2-hydroxy-6-methoxy- and 2,6-dimethoxyacetophenones.

A Bobik, G M Holder, A J Ryan, L I Wiebe

文献索引：Xenobiotica 5(2) , 65-72, (1975)

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摘要

1. 2,6-Dihydroxyacetophenone, its mono- and di-methyl ethers are inhibitors of hepatic mixed function oxidases. The dimethyl ether is a competitive inhibitor of aminopyrine demethylase with the others displaying mixed kinetics. The metabolism of all three ketones has been studied. 2. 2,6-Dihydroxyacetophenone is excreted unchanged and as conjugates. 3. 2-Hydroxy-6-methoxyacetophenone is largely excreted unchanged and conjugated but small amounts of the 3- and 5-hydroxylated derivatives are formed. 4. 2,6-Dimethoxyacetophenone is demethylated to 2-hydroxy-6-methoxy-acetophenone. In addition 3-hydroxy-2,5-dimethoxyacetophenone and 2,3-dihydroxy-6-methoxyacetophenone were identified as metabolites. 5. Quantitative data on the excretion of metabolites were obtained with 14C-labelled ketones.