Valcavi U, Caponi R, Martelli P, Minoja F
Eur J Drug Metab Pharmacokinet. 1979;4(4):231-5. doi: 10.1007/BF03189432.
The metabolism of the hypolipemic agent 3-methyl-4-phenyl-3-butenoic acid diethylamide (I) after oral administration to rabbits has been qualitatively investigated. Four main metabolites were identified in the urine of animals deriving from three different metabolic processes: aromatic hydroxylation, lactonization and N-dealkylation. All metabolites occured in free forms, were pharmacologically inactive and the unchanged starting drug was never recovered. The metabolic pathway of compound I was also compared with that of the parent non-substituted amide, 3-methyl-4-phenyl-3-butenamide (II). The fate of the two structurally related drugs was similar, except for hydroxylation of the carbon in the alpha position to the amidic group, occuring in compound II but not in compound I.
对降血脂药物3-甲基-4-苯基-3-丁烯酸二乙酰胺（I）口服给予兔子后的代谢情况进行了定性研究。在动物尿液中鉴定出四种主要代谢产物，它们源自三种不同的代谢过程：芳香族羟基化、内酯化和N-脱烷基化。所有代谢产物均以游离形式存在，无药理活性，且从未回收得到未变化的起始药物。还将化合物I的代谢途径与母体非取代酰胺3-甲基-4-苯基-3-丁烯酰胺（II）的代谢途径进行了比较。这两种结构相关药物的代谢情况相似，只是在酰胺基团α位的碳原子羟基化方面有所不同，化合物II会发生这种羟基化，而化合物I则不会。
