Befunolol代謝活性の種差に関するin Vitro研究

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The species differences in the metabolism of befunolol were investigated by using the cell fractions prepared from the liver or other tissues of several species. 2-Carbonyl-reducing activity forming 2-(1-hydroxyethyl)-7-(2-hydroxy-3-isopropylaminopropoxy) benzofuran (MI) was detected in the hepatic 103500×g supernatant from human and experimental animals such as rabbit, rat, hamster, guinea pig and mouse. 4-Hydroxylating activity forming 2-acetyl-4-hydroxy-7-(2-hydroxy-3-isopropylaminopropoxy) benzofuran (M II) and oxidizing activity at 7-side chain of befunolol were detected in the hepatic microsomal fraction from the animals, but not in that from human. The differences among the species were observed in the degree of each befunolol-metabolizing activity. The reducing activity in the animals was inhibited by the presence of microsome, but the activity in human did not vary under similar conditions. At low concentration of befunolol, the 9000×g supernatant of the human liver in which neither 4-hydroxylating nor 7-side chain oxidizing activity was detected apparently showed higher reducing activity than that of the animals. The reducing activity was detected in the cell fraction of several organs besides liver. The species differences in the pattern of tissue distribution of the activity were also observed among rabbit, guinea pig and human.
公益社団法人日本薬学会の論文
1980-09-25