Results 231 to 240 of about 27,101 (273)
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Phenobarbital N-glucosylation by human liver microsomes
European Journal of Drug Metabolism and Pharmacokinetics, 2004Glucosylation of xenobiotics in mammals has been observed for a limited number of drugs. Generally, these glucoside conjugates are detected as urinary excretion products with limited information on their formation. An in vitro assay is described for measuring the formation of the phenobarbital N-glucoside diasteriomers ((5R)-PBG, (5S)-PBG) using human ...
Sheela G, Paibir +3 more
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Biotransformation of 1,8-Cineole by Human Liver Microsomes
Natural Product Letters, 2001The biotransformation of 1,8-cineole has been investigated by using human liver microsomes. A single oxidized metabolite, 2-exo-hydroxy-1,8-cineole, was isolated. Its formation was investigated under various conditions by changing incubation time, P450 level in liver microsomes, and substrate concentration.
M, Miyazawa, M, Shindo
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Bioactivation of Flutamide Metabolites by Human Liver Microsomes
Drug Metabolism and Disposition, 2008Flutamide, a widely used nonsteroidal antiandrogen drug for the treatment of prostate cancer, has been associated with rare incidences of hepatotoxicity in patients. It is believed that bioactivation of flutamide and subsequent covalent binding to cellular proteins is responsible for its toxicity. A novel N-S glutathione adduct has been identified in a
Ping, Kang +5 more
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In Vitro Metabolism of Flucetosulfuron by Human Liver Microsomes
Journal of Agricultural and Food Chemistry, 2014To investigate herbicide metabolism, human liver microsomes were incubated with threo- and erythro-isomers of flucetosulfuron. Each isomer produced one metabolite; the metabolites were unambiguously identified as enzymatic hydrolysis products by using liquid chromatography-tandem mass spectrometry (LC-MS/MS).
Yong-Sang, Lee +7 more
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Metabolism of benz[a]anthracene by human liver microsomes
Cancer Letters, 1994The metabolism of benz[a]anthracene (BA) by human hepatic microsomes was investigated. Only dihydrodiols were observed when BA was the substrate. No tetrahydrotetrols were detected, indicating lack of diol epoxide formation. The BA-dihydrodiols identified by GCMS analysis and comparison to authentic standards were BA-8,9-dihydrodiol (42.4% of total ...
Y, Sahali +3 more
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Drug Metabolism and Disposition, 2011
Raloxifene, a selective estrogen receptor modulator, exhibits quite large interindividual variability in pharmacokinetics and pharmacodynamics. In women, raloxifene is metabolized extensively by different isoforms of UDP-glucuronosyltransferase (UGT) to its glucuronides.
Tina, Trdan Lusin +2 more
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Raloxifene, a selective estrogen receptor modulator, exhibits quite large interindividual variability in pharmacokinetics and pharmacodynamics. In women, raloxifene is metabolized extensively by different isoforms of UDP-glucuronosyltransferase (UGT) to its glucuronides.
Tina, Trdan Lusin +2 more
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Characterization of fimasartan metabolites in human liver microsomes and human plasma
Xenobiotica, 20151. The metabolites of fimasartan (FMS), a new angiotensin II receptor antagonist, were characterized in human liver microsomes (HLM) and human subjects. 2. We developed a method for a simultaneous quantitative and qualitative analysis using predictive multiple reaction monitoring information-dependent acquisition-enhanced product ion scanning.
Ji-Yoon, Lee +11 more
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Chemico-Biological Interactions, 2011
Anthracyclines (ANTs) are widely used in the treatment of various forms of cancer. Although their usage contributes to an improvement in life expectancy, it is limited by severe adverse effects-acute and chronic cardiotoxicity. Several enzymes from both AKR and SDR superfamilies have been reported as participants in the reduction of ANTs.
Adam, Skarka +3 more
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Anthracyclines (ANTs) are widely used in the treatment of various forms of cancer. Although their usage contributes to an improvement in life expectancy, it is limited by severe adverse effects-acute and chronic cardiotoxicity. Several enzymes from both AKR and SDR superfamilies have been reported as participants in the reduction of ANTs.
Adam, Skarka +3 more
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Metabolism of coumarin by rat, gerbil and human liver microsomes
Xenobiotica, 19921. o-Hydroxyphenylacetaldehyde was the major metabolite of coumarin (1 mM) in rat, gerbil and human liver microsomes. 2. Treatment of rats with phenobarbitone (PB) or beta-naphthoflavone increased the o-hydroxyphenylacetaldehyde formed. 3-Hydroxycoumarin was the other main metabolite produced by rat liver microsomes. 3.
J H, Fentem, J R, Fry
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Enantioselective Metabolism of Mefentrifluconazole by Human Liver Microsomes
Journal of Agricultural and Food ChemistryA better understanding of the metabolic differences between chiral pesticide enantiomers in organisms is crucial for accurately assessing their risk. The enantioselective metabolism of mefentrifluconazole was investigated by the human liver microsome reaction system.
Yuqi Ren +6 more
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