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Glucuronidation of 7-hydroxy-4-methylcoumarin by human liver microsomes. Inhibition by certain drugs.

作者信息

Irshaid Y M, Gharaybeh K I, Ammari F F, Rawashdeh N M

机构信息

Faculty of Medicine, Jordan University of Science and Technology, Irbid.

出版信息

Eur J Drug Metab Pharmacokinet. 1990 Oct-Dec;15(4):295-301. doi: 10.1007/BF03190218.

DOI:10.1007/BF03190218
PMID:2128479
Abstract

Glucuronidation of 7-hydroxy-4-methylcoumarin (7-OH-4-MC) was comparable in three of the four human liver samples studied. In liver sample IV the glucuronidation rate of 7-OH-4-MC was almost 40% of that in the other samples. That might be due to interindividual variation in the capacity to glucuronidate. Glucuronidation rates were not reduced in the one human liver sample which displayed mild centrilobular cholestasis on histopathology. Furosemide (FR), salicylic acid (SA), lorazepam (Z) and menthol (MT) inhibited the glucuronidation of 7-OH-4-MC to varying degrees (30-90%). Paracetamol (PA) and 5-hydroxytryptamine (HT) were not inhibitors of the glucuronidation of 7-OH-4-MC. These findings suggest the presence of other UDP-glucuronosyltransferase (UDPGT) isozymes in the human liver microsomes which are responsible for the glucuronidation of PA and HT than those which glucuronidate 7-OH-4-MC.

摘要

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本文引用的文献

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Differential effects of oral contraceptive steroids on the metabolism of benzodiazepines.口服避孕药类固醇对苯二氮䓬类药物代谢的不同影响。
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Paracetamol as a test drug to determine glucuronide formation in man. Effects of inducers and of smoking.对乙酰氨基酚作为一种测试药物用于确定人体中葡萄糖醛酸苷的形成。诱导剂和吸烟的影响。
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Glucuronidation of 7-hydroxycoumarin in periportal and pericentral regions of the lobule in livers from untreated and 3-methylcholanthrene-treated rats.未处理和经3-甲基胆蒽处理的大鼠肝脏小叶门周区和中央周区中7-羟基香豆素的葡萄糖醛酸化作用
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Mol Pharmacol. 1987 Jan;31(1):27-34.
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A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.一种利用蛋白质 - 染料结合原理对微克级蛋白质进行定量的快速灵敏方法。
Anal Biochem. 1976 May 7;72:248-54. doi: 10.1016/0003-2697(76)90527-3.