Results 201 to 210 of about 50,120 (254)

Phenobarbital N-glucosylation by human liver microsomes

European Journal of Drug Metabolism and Pharmacokinetics, 2004
Glucosylation 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, William H, Soine, Diana F, Thomas, Robert A, Fisher   +3 more
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Microsomal Esterification of Retinol in Human Liver

Acta Medica Scandinavica, 1984
Abstract Recent work has shown that esterification of retinol in microsomes from rat liver, mammary gland and small intestine and from human small intestine is catalyzed by an acyl CoA: retinol acyl transferase (ARAT). The current study demonstrates ARAT activity in human liver microsomes.
M, Rasmussen, P, Helgerud, L B, Petersen, K R, Norum   +3 more
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REDUCTION OF 3-OXOSTEROIDS IN HUMAN LIVER MICROSOMES

Acta Endocrinologica, 1976
ABSTRACT The 3α- and 3β-reduction of the following steroids was studied in human liver microsomes: 5α-androstane-3,17-dione, 17β-hydroxy-5α-androstan-3-one, 5α-pregnane-3,20-dione, 5β-pregnane-3,20-dione, 3-oxo-5β-cholanoic acid and 7α-hydroxy-5α-cholestan-3-one.
I, Björkhem, K, Einarsson, G, Hellers, K, Wikvall   +3 more
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Metabolism of Ketamine Stereoisomers by Human Liver Microsomes

Anesthesiology, 1992
Ketamine is used clinically as a racemic mixture of optical isomers that differ in their analgesic properties and psychomimetic effects. Administered individually, or together as the racemate, ketamine enantiomers differ in their hepatic clearance and duration of anesthetic effect.
E D, Kharasch, R, Labroo
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Aminopyrine N-demethylase activity in human liver microsomes

Clinical Pharmacology and Therapeutics, 1990
Aminopyrine N-demethylase activity and the contents of cytochrome P-450, cytochrome b5, and NADPH-reductase activity in human liver microsomes from 31 different patients were studied. Our results show the existence of significant interindividual, but not sex- or age-related differences in N-demethylase activity (ranging between 0.52 and 4.42 nmol/min ...
J A, García-Agúndez, A, Luengo, J, Benítez   +2 more
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Characterization of metronidazole metabolism by human liver microsomes

Biochemical Pharmacology, 1991
The metabolism of metronidazole was studied in microsomes isolated from livers of human kidney donors. The formation of the major in vivo metabolite, hydroxymetronidazole, proceeded according to biphasic kinetics, suggesting the involvement of at least two enzymatic sites.
S, Loft, S V, Otton, M S, Lennard, G T, Tucker, H E, Poulsen   +4 more
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Bioactivation of Flutamide Metabolites by Human Liver Microsomes

Drug Metabolism and Disposition, 2008
Flutamide, 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, Deepak, Dalvie, Evan, Smith, Sue, Zhou, Alan, Deese, James A, Nieman   +5 more
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Biotransformation of 1,8-Cineole by Human Liver Microsomes

Natural Product Letters, 2001
The 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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Flavin-Containing Monooxygenase Activity in Human Liver Microsomes

1986
Human liver microsomal flavin-containing monooxygenase activity has been studied using dimethylaniline N-oxidation and thiobenzamide S-oxidation. Except for one subject, the capacity of human liver microsomes to mediate these reactions were markedly increased at pH 8.4 compared to pH 7.4.
M E, McManus, D J, Birkett, W M, Burgess, I, Stupans, J A, Koenig, A R, Boobis, D S, Davies, P J, Wirth, P H, Grantham, S S, Thorgeirsson   +9 more
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The metabolism of tramadol by human liver microsomes

The Clinical Investigator, 1992
The metabolism of tramadol was investigated in vitro using microsomal fractions of human liver. The parent compound and its main metabolites were determined by a newly developed high performance liquid chromatography assay. O-demethylation of tramadol was found to be stereoselective. The Vmax of the O-demethylation of (-)-tramadol was 210 pmol.mg-1.min-
W D, Paar, P, Frankus, H J, Dengler
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