Results 211 to 220 of about 50,120 (254)

Human liver microsomal thiol methyltransferase: inhibition by arylalkylamines

Xenobiotica, 1993
1. Thiol methyltransferase (TMT) is a microsomal enzyme catalyzing the S-methylation of aliphatic sulphydryl drugs and xenobiotics. Studies of the functional significance of S-methylation catalysed by TMT have been hampered by lack of a potent, relatively specific, non-toxic inhibitor of the enzyme. 2.
T A, Glauser, E, Saks, V M, Vasova, R M, Weinshilboum   +3 more
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Δ2-Valproate biotransformation using human liver microsomal fractions

Pharmaceutisch Weekblad Scientific Edition, 1992
The metabolism of 2-n-propyl-2-pentenoate (delta 2-VPA) was evaluated in human hepatic microsomal fractions. Two biotransformation pathways have been particularly investigated. In the presence of the cytochrome P-450 co-factor, NADPH, the main metabolites recovered were delta 3-VPA, delta 2,4-VPA and VPA.
G, Fabre, C, Briot, E, Marti, J P, Montseny, M, Bourrié, D, Massé, Y, Berger, J P, Cano   +7 more
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CYP2C19 Participates in Tolbutamide Hydroxylation by Human Liver Microsomes

Drug Metabolism and Disposition, 2000
Tolbutamide is a sulfonylurea-type oral hypoglycemic agent whose action is terminated by hydroxylation of the tolylsulfonyl methyl moiety catalyzed by cytochrome P-450 (CYP) enzymes of the human CYP2C subfamily. Although most studies have implicated CYP2C9 as the exclusive catalyst of hepatic tolbutamide hydroxylation in humans, there is evidence that ...
M R, Wester, J M, Lasker, E F, Johnson, J L, Raucy   +3 more
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Drug Interactions of Paclitaxel Metabolism in Human Liver Microsomes

Journal of Chemotherapy, 2003
The human liver metabolism of paclitaxel (Taxol), an anticancer drug, leads to three metabolites: 6alpha-hydroxypaclitaxel, 3'-p-hydroxypaclitaxel and 6alpha,3'-p-dihydroxypaclitaxel. The inter-individual variability of paclitaxel metabolism was investigated first in vitro using 22 human liver microsomes.
S S, Bun, J, Ciccolini, H, Bun, C, Aubert, J, Catalin   +4 more
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Enantioselective Metabolism of Mefentrifluconazole by Human Liver Microsomes

Journal of Agricultural and Food Chemistry
A 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, Peilin Guo, Xinglu Pan, Jun Xu, Xiaohu Wu, Yongquan Zheng, Fengshou Dong   +6 more
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Predicting human liver microsomal stability with machine learning techniques

Journal of Molecular Graphics and Modelling, 2008
To ensure a continuing pipeline in pharmaceutical research, lead candidates must possess appropriate metabolic stability in the drug discovery process. In vitro ADMET (absorption, distribution, metabolism, elimination, and toxicity) screening provides us with useful information regarding the metabolic stability of compounds.
Yojiro, Sakiyama, Hitomi, Yuki, Takashi, Moriya, Kazunari, Hattori, Misaki, Suzuki, Kaoru, Shimada, Teruki, Honma   +6 more
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Enantioselective carbonyl reduction of eperisone in human liver microsomes

Xenobiotica, 2011
Eperisone, 4-ethyl-2-methyl-3-piperidinopropiophenone, is a centrally acting muscle relaxant widely used to relieve muscle stiffness and back pain. In this study, enantioselectivity for carbonyl reduction of eperisone was investigated in human liver microsomes, and the enzymes involved in the carbonyl reduction were characterised. Carbonyl reduction of
Hye Hyun, Yoo, Nam-Sun, Kim, Min Jung, Kim, Dongyun, Shin, Jae-Gook, Shin, Dong-Hyun, Kim   +5 more
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Gender difference in ifosfamide metabolism by human liver microsomes

European Journal of Drug Metabolism and Pharmacokinetics, 2001
Pharmacokinetic gender-dependent differences in cytochrome P450-mediated drug metabolism, especially CYP3A4, and their clinical implications are increasingly apparent. CYP3A4 seems to be the most important CYP isoform in both bioactivation and N-dechloroethylation of the alkylating prodrug ifosfamide, but informations about possible gender-related ...
R, Schmidt, F, Baumann, H, Hanschmann, F, Geissler, R, Preiss   +4 more
openaire   +2 more sources

Piperazinyl CCR1 antagonists—optimization of human liver microsome stability

Bioorganic & Medicinal Chemistry Letters, 2007
The synthesis, biological activity, and pharmacokinetic profile of CCR1 antagonists are described.
Matthew F, Brown, Kevin B, Bahnck, Laura C, Blumberg, William H, Brissette, Sara A, Burrell, James P, Driscoll, Flavia, Fedeles, Michael B, Fisher, Robert S, Foti, Ronald P, Gladue, Aikomari, Guzman-Martinez, Matthew M, Hayward, Paul D, Lira, Brett M, Lillie, Yi, Lu, Greg D, Lundquist, Eric B, McElroy, Molly A, McGlynn, Timothy J, Paradis, Christopher S, Poss, James H, Roache, Andrei, Shavnya, Richard M, Shepard, Kristen A, Trevena, Laurie A, Tylaska   +24 more
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Lidocaine metabolism in human liver microsomes by cytochrome P450IIIA4

Clinical Pharmacology and Therapeutics, 1989
The metabolism of lidocaine to its major metabolite monoethylglycinexylidide (MEGX) was studied in human liver microsomes of 13 kidney transplant donors and of one patient with liver cirrhosis. Interindividual variation in metabolite formation was considerable.
M J, Bargetzi, T, Aoyama, F J, Gonzalez, U A, Meyer   +3 more
openaire   +2 more sources