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奎尼丁和奎宁对人和大鼠肝微粒体氧化酶的抑制作用

Inhibitory effects of quinidine and quinine on liver microsome oxidation enzymes in man and rat 1
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摘要 奎尼丁和奎宁对人和大鼠肝微粒体氧化酶的抑制作用1涂植光,赵梁立2(重庆医科大学临床生化教研室,2药理教研室,重庆630046,中国)关键词奎尼丁;奎宁;肝微粒体;遗传药理学;丁呋洛尔;烃基香豆素脱烃基酶;芳基烃羟化酶类目的:比较奎尼丁和奎宁对人和大鼠... IM: To compare the inhibitory effects of quinidine and quinine on liver microsome bufuralol 1′ hydroxylase (BH), aryl hydrocarbon hydroxyl ̄ase (AHH), and 7 ethoxycoumarin O deethyl ̄ase (ED) activities in man and rat. METHODS: A normal phase HPLC and the fluorescence spectrometry were used to assay the enzyme activities. RESULTS: Both quinidine and quinine produced a concentration dependent inhibition to liver microsome BH, AHH, and ED in man and rat. Their median inhibitory concentrations (IC 50 ) on liver microsome BH, AHH, and ED low and high affinity phases were 0 2, 378, 2952, and >5000 μmol·L -1 for quinine in man, 290, 613, 1465, 1595, μmol·L -1 for quinidine in rat; 29, 207, 808, and >5000 μmol·L -1 for quinine in man, and 31, 54, 597, and 2508 μmol·L -1 for quinine in rat, respectively. CONCLUSION: Quinidine is a species and stereo selective potent inhibitor to human liver microsome BH.
出处 《中国药理学报》 CSCD 1996年第6期541-544,共4页 Acta Pharmacologica Sinica
基金 the Youth Funds of State Educational Commission
关键词 奎尼丁 奎宁 肝微粒体 遗传药理学 氧化酶 quinidine quinine liver micro ̄somes pharmacogenetics bufuralol 7 alkoxy ̄cou ̄marin O dealkylase aryl hydrocarbon hydroxylases
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参考文献3

  • 1涂植光,中国药理学报,1995年,16卷,325页
  • 2Zhou H H,Clin Pharmacol Ther,1990年,47卷,686页
  • 3涂植光,中国药理学报,1989年,10卷,465页

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