Teshima R, Nagamatsu K, Ikebuchi H, Kido Y, Terao T
Drug Metab Dispos. 1983 Mar-Apr;11(2):152-7.
The metabolism of 2-methylnaphthalene (2-MN) in guinea pigs (in vivo and in vitro) was investigated. Excretion of 2-MN from guinea pigs took place rapidly. In the first 24 hr, nearly 80% of the orally administered 2-[3H]-MN was excreted in the urine in the form of several metabolites, and about 10% of it was recovered in the feces. The major metabolites in the urine were oxidative products of the methyl group of 2-MN (naphthoic acid and its glycine and glucuronic acid conjugates) and accounted for 76% of the total urinary radioactivity in the first 24 hr. S-(7-Methyl-1-naphthyl)cysteine and glucuronic acid and sulfate conjugates of 7-methyl-1-naphthol were also identified as minor metabolites (18% of the total urinary radioactivity). As an in vitro metabolite, the formation of S-(7-methyl-1-naphthyl)glutathione was indicated using the 9,000g supernatant of the homogenate of guinea pig liver. The oral administration of 2-MN (500 mg/kg) to guinea pigs significantly lowered the trichloroacetic acid-soluble sulfhydryl content in the liver.
研究了豚鼠体内和体外2-甲基萘(2-MN)的代谢情况。豚鼠对2-MN的排泄迅速。在最初的24小时内,口服给予的2-[3H]-MN中近80%以几种代谢物的形式经尿液排泄,约10%经粪便回收。尿液中的主要代谢物是2-MN甲基的氧化产物(萘甲酸及其甘氨酸和葡萄糖醛酸结合物),在最初24小时内占尿液总放射性的76%。S-(7-甲基-1-萘基)半胱氨酸以及7-甲基-1-萘酚的葡萄糖醛酸和硫酸盐结合物也被鉴定为次要代谢物(占尿液总放射性的18%)。作为体外代谢物,使用豚鼠肝脏匀浆的9000g上清液表明形成了S-(7-甲基-1-萘基)谷胱甘肽。给豚鼠口服2-MN(500mg/kg)显著降低了肝脏中三氯乙酸可溶性巯基含量。