Results 181 to 190 of about 287,149 (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
openaire   +2 more sources

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
openaire   +2 more sources

In vitro glucuronidation using human liver microsomes and the pore-forming peptide alamethicin.

Drug Metabolism And Disposition, 2000
The UDP-glucuronosyltransferases (UGTs) are a superfamily of membrane-bound enzymes whose active site is localized inside the endoplasmic reticulum.
M. Fisher, K. Campanale, B. Ackermann, M. Vandenbranden, S. Wrighton   +4 more
semanticscholar   +1 more source

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
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

Interindividual variability in acetaminophen glucuronidation by human liver microsomes: identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms.

Journal of Pharmacology and Experimental Therapeutics, 2001
Interindividual variability in acetaminophen (APAP) glucuronidation may contribute to differences in susceptibility to APAP intoxication in humans.
M. Court, S. Duan, L. Moltke, D. Greenblatt, C. Patten, J. Miners, P. Mackenzie   +6 more
semanticscholar   +1 more source

Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes.

Journal of Pharmacology and Experimental Therapeutics, 1996
The HIV-1 protease inhibitor ritonavir (ABT-538) undergoes cytochrome P450-mediated biotransformation in human liver microsomes to three major metabolites, Ml, M2 and M11, with wide interindividual variation in the rates of metabolite formation.
Gondi N. Kumar, A. D. Rodrigues, A. Buko, J. Denissen   +3 more
semanticscholar   +1 more source