Results 191 to 200 of about 287,149 (254)

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

Characterization of CYP2A6 involved in 3'-hydroxylation of cotinine in human liver microsomes.

Journal of Pharmacology and Experimental Therapeutics, 1996
Nicotine is primarily metabolized to cotinine, and cotinine is further metabolized to trans-3'-hydroxycotinine in human liver, which is a major metabolite of nicotine in humans.
M. Nakajima, Toshinori Yamamoto, K. Nunoya, T. Yokoi, K. Nagashima, Kazuhide Inoue, Y. Funae, Noriaki Shimada, Tetsuya Kamataki, Yukio Kuroiwa   +9 more
semanticscholar   +1 more source

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
openaire   +2 more sources

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

Variation in glucuronidation of lamotrigine in human liver microsomes

Xenobiotica, 2009
Lamotrigine (LTG), a diaminotriazine anti-epileptic, is principally metabolized at the 2-position of the triazine ring to form a quaternary ammonium glucuronide (LTGG) by uridine glucuronosyl transferease (UGT) 1A3 and UGT1A4. It has been hypothesized that glucuronidation of anti-epileptic drugs is spared with age, despite a known decrease in liver ...
U A, Argikar, R P, Remmel
openaire   +2 more sources

FACTORS INFLUENCING MIDAZOLAM HYDROXYLATION ACTIVITY IN HUMAN LIVER MICROSOMES

Drug Metabolism and Disposition, 2006
The cytochrome P450 3A (CYP3A) subfamily (mainly CYP3A4 and CYP3A5) is responsible for metabolizing approximately half of currently marketed drugs, but with considerable interindividual variability in expression and function. To investigate factors contributing to this variability, rates of midazolam (MDZ) 1'-hydroxylation and CYP3A4 and CYP3A5 protein
Ping, He, Michael H, Court, David J, Greenblatt, Lisa L, von Moltke   +3 more
openaire   +2 more sources

Characterization of 1′-Hydroxymidazolam Glucuronidation in Human Liver Microsomes

Drug Metabolism and Disposition, 2008
Midazolam is a potent benzodiazepine derivative with sedative, hypnotic, anticonvulsant, muscle-relaxant, and anxiolytic activities. It undergoes oxidative metabolism catalyzed almost exclusively by the CYP3A subfamily to a major metabolite, 1'-hydroxymidazolam, which is equipotent to midazolam.
Bing, Zhu, David, Bush, George A, Doss, Stella, Vincent, Ronald B, Franklin, Shiyao, Xu   +5 more
openaire   +2 more sources

Metabolism of benz[a]anthracene by human liver microsomes

Cancer Letters, 1994
The 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, L R, Kidd, P L, Skipper, S R, Tannenbaum   +3 more
openaire   +2 more sources

Lindane metabolism by human and rat liver microsomes^†

Xenobiotica, 1982
1. Human liver microsomes convert lindane (gamma isomer of 1,2,3,4,5,6-hexachlorocyclohexane) to four major primary metabolites; gamma-1,2,3,4,5,6-hexachlorocyclohex-1-ene (3,6/4,5-HCCH), gamma-1,3,4,5,6-pentachlorocyclohex-1-ene (3,6/4,5-PCCH), beta-1,3,4,5,6-pentachlorocyclohex-1-ene (3,4,6/5-PCCH), and 2,4,6-trichlorophenol (2,4,6-TCP); and two ...
J F, Fitzloff, J, Portig, K, Stein
openaire   +2 more sources

NADPH-Dependent Metabolism of Estrone by Human Liver Microsomes

The Journal of Pharmacology and Experimental Therapeutics, 2002
We characterized the NADPH-dependent metabolism of estrone (E1) by liver microsomes of 21 male and 12 female human subjects. The structures of 11 hydroxylated or keto metabolites of E1 formed by human liver microsomes were identified by chromatographic and mass spectrometric analyses.
Anthony J, Lee, Laura H, Mills, Joseph W, Kosh, Allan H, Conney, Bao Ting, Zhu   +4 more
openaire   +2 more sources