Honda T, Fukada A, Kiyozumi M, Kojima S
Eur J Drug Metab Pharmacokinet. 1987 Jan-Mar;12(1):11-6. doi: 10.1007/BF03189856.
Four unconjugated metabolites, which were produced through the oxidation of the isopropyl chain of 2-isopropylnaphthalene (2-IPN), were isolated from the urine of rabbits receiving 2-IPN orally and identified: 2-(2-naphthyl)propionic acid, 2-(2-naphthyl)-2-propanol, 2-(2-naphthyl)-1,2-propanediol, and 2-(2-naphthyl)-2-hydroxypropionic acid, together with a small amount of the unchanged compound. Further, the unconjugated metabolites, which were produced through the oxidation of the naphthalene ring, were isolated and identified: 2-isopropylnaphthols and 2-isopropyl-5,6 (or 7,8)-dihydronaphthalene-5,6 (or 7,8)-diol. The identification of these metabolites was made by means of TLC, GLC, MS, IR, GC/MS, and FT-NMR. The presence of glucuronides of metabolites B, C, D, F, and H was also suggested by TLC and GLC of the extract obtained after hydrolysis by beta-glucuronidase. In addition, quantitative determination of the metabolites indicated that the total urinary excretion of the metabolites except 2-isopropylnaphthols in 24 hr after administration was about 29% of the dose.
从经口给予2-异丙基萘(2-IPN)的家兔尿液中分离并鉴定出四种通过2-异丙基萘异丙基链氧化产生的非共轭代谢物:2-(2-萘基)丙酸、2-(2-萘基)-2-丙醇、2-(2-萘基)-1,2-丙二醇和2-(2-萘基)-2-羟基丙酸,以及少量未变化的化合物。此外,还分离并鉴定了通过萘环氧化产生的非共轭代谢物:2-异丙基萘酚和2-异丙基-5,6(或7,8)-二氢萘-5,6(或7,8)-二醇。这些代谢物通过薄层色谱法(TLC)、气相色谱法(GLC)、质谱法(MS)、红外光谱法(IR)、气相色谱-质谱联用法(GC/MS)和傅里叶变换核磁共振法(FT-NMR)进行鉴定。通过β-葡萄糖醛酸酶水解后提取物的TLC和GLC也表明存在代谢物B、C、D、F和H的葡萄糖醛酸苷。此外,代谢物的定量测定表明,给药后24小时内除2-异丙基萘酚外的代谢物总尿排泄量约为剂量的29%。