チオ尿素誘導体の代謝に関する研究(第3報) : N-Methylthiocarbanilideの水酸化誘導体の家兎における代謝について

抄録

The metabolism of three hydroxylated derivatives of N-methylthiocarbanilide, namely, 4'-hydroxy-, 4-hydroxy-, and 4, 4'-dihvdroxy-N-methylthiocarbanilide, was studied. Examinations were made on the urinary metabolites in rabbits after oral administration of these compounds, tested by paper and thin-layer chromatography. The major metabolism of the respective derivatives is summarized as follows. 1) The fate of 4'-hydroxy derivative is quite similar to that of N-methylthiocarbanilide. Its main metabolite is the glucuronide at the 4'-hydroxyl group and the sulfuric acid conjugation was not observed. 2) The metabolism of 4-hydroxy derivative is different from that of 4'-hydroxy derivative since the former is conjugated with both glucuronic acid and sulfuric acid at the 4-hydroxyl group. In addition the glucuronide of p-methylaminophenol is also excreted. 3) 4, 4'-Dihydroxy derivative is excreted mainly as the monoglucuronide in which the conjugation occurs exclusively at the 4'-hydroxyl group and the ethereal sulfate was not detected.