医薬品の生体内変化に関する研究(第58報) : 4-ブチルアミノアンチピリンの生体内変化について

概要

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In the metabolic study of butyl aryl ethers in vivo, it has been shown in this laboratory that dealkylation is only minor and penultimate hydroxylation is the major one. In connection with this study, metabolism of 4-butylaminoantipyrine was investigated to learn whether it also undergoes the penultimate hydroxylation rather than the dealkylation of butyl chain. Contrary to this expectation, the major pathway of this drug was found to be dealkylation in all of the animals tested (rabbits, guinea pigs, mice, and rats), excreting 4-aminoantipyrine and its acetylated metabolite, 4-acetamidoantipyrine, as the main metabolites. However, it has also been recognized that there is a small amount of other urinary metabolite. The structure of this minor metabolite has been identified as 4-(2-butenylamino)antipyrine by the comparison with the authentic sample chemically synthesized. Since it seems very likely that this metabolite may be formed from the penultimate hydroxylated metabolite by dehydration, the presnet study would support the hypothesis that, as in C- and O-alkyl compounds, the penultimate hydroxylation takes place also in N-alkyl compounds if they have a considerably long alkyl chain such as butyl group.
社団法人日本薬学会の論文
1968-01-25