INHIBITION BY SKF 525-A OF 7-ETHOXYCOUMARIN O-DEETHYLATION IN MICROSOMAL AND THE RECONSTITUTED MONOOXYGENASE SYSTEMS FROM PCB-TREATED RAT LIVERS
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概要
- 論文の詳細を見る
Addition of diethylaminoethyl 2, 2-diphenylvalerate-HCl (SKF 525-A) to the incubation mixture containing liver microsomes or purified cytochrome P-450 (PCB P-450) from PCB (KC-500)-treated rats resulted in non-competitive inhibition of 7-ethoxycoumarin O-deethylation activity whereas the addition to the incubation mixture containing purified cytochrome P-448 (PCB P-448) showed a competitive inhibition. Fortification of PCB-induced microsomes with purified NADPH—cytochrome P-450 reductase enhanced the O-deethylation activity. With the reductase-fortified microsomes, SKF 525-A inhibited the O-deethylation in a competitive manner. Based on these results, we confirmed that SKF 525-A inhibits non-competitively and competitively, depending on the species of cytochrome P-450. Our results also support the view that in microsomes from PCB-treated rats, PCB P-450 rather than PCB P-448 is mainly involved in the O-deethylation reaction, presumably due to the presence of a limited amount of NADPH—cytochrome P-450 reductase in microsomes.
- 社団法人 日本薬理学会の論文
著者
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KAMATAKI TETSUYA
Department of Pharmacology, School of Medicine, Keio University
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Kato Ryuichi
Department Of Biology Graduate School Of Science Osaka University
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Kamataki Tetsuya
Department Of Pharmacology School Of Medicine Keio University:department Of Analytical Biochemistry
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Kamataki Tetsuya
Department Of Biochemical Pharmacology Faculty Of Pharmaceutical Sciences Chiba University
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Ishii Kenji
Department Of Agricultural And Biological Chemistry Nihon University
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Ando Mebae
Department Of Pharmacology School Of Medicine Keio University
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KAMATAKI Tetsuya
Department of Analytical Bio chemistry, School of Pharmacy, Hokkaido University
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