نتایج جستجو برای: ژن cyp2d6

تعداد نتایج: 18157  

Journal: :The Journal of pharmacology and experimental therapeutics 2001
B J Ring J A Eckstein J S Gillespie S N Binkley M VandenBranden S A Wrighton

The formation of R- and S-norfluoxetine was analyzed in vitro in human liver microsomes. Low apparent K(m) values for R-norfluoxetine formation of < or =8 microM and S-norfluoxetine of <0.2 microM were determined. R-Norfluoxetine formation rates in a characterized microsomal bank correlated with the catalytic activities for cytochrome P450 (CYP) 2D6, CYP2C9, and CYP2C8. Expressed CYP2C9, CYP2C1...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2001
J R Palamanda C N Casciano L A Norton R P Clement L V Favreau C Lin A A Nomeir

SCH 66712 [5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine] caused a time- and NADPH-dependent loss of CYP2D6 activity. The inactivation of human liver (HL) microsomal dextromethorphan O-demethylase activity, a prototype marker for CYP2D6, was characterized by a K(I) of 4.8 microM and a maximal rate constant of inactivation (k(inact)) of 0.14 min(-1). The inactivation...

Journal: :Polish journal of pharmacology 2004
Anna Haduch Jacek Wójcikowski Władysława A Daniel

The aim of the present work was to study the effect of chronic treatment with pharmacological doses of selected antidepressants (imipramine, mirtazapine) and neuroleptics (thioridazine, risperidone) on the activity and level of CYP2D in the rat brain. Our previous studies carried out on the liver showed that after chronic treatment with psychotropics, the activity of CYP2D was significantly dec...

2011
Jadwiga Skrętkowicz Małgorzata Barańska Anna Kaczorowska Mariola Rychlik-Sych

INTRODUCTION Systemic lupus erythematosus (SLE) is a complex, multifactor autoimmune disease. The studies on aetiopathogenesis of autoimmune diseases focus on the impact the genetically conditioned impairment of xenobiotic metabolism may exert. The knowledge of oxidation polymorphism in the course of SLE may be helpful in choosing more efficient and safer therapy. We determined whether there wa...

2014
Kristin Dickschen Thomas Eissing Thomas Mürdter Matthias Schwab Stefan Willmann Georg Hempel

PURPOSE To overcome cytochrome P450 2D6 (CYP2D6) mediated tamoxifen resistance in postmenopausal early breast cancer, CYP2D6 phenotype-adjusted tamoxifen dosing in patients with impaired CYP2D6 metabolism and/or the application of endoxifen, the most potent tamoxifen metabolite, are alternative treatment options. To elucidate both strategies comprehensively we used a physiologically-based pharm...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2009
Laura K Chico Heather A Behanna Wenhui Hu Guifa Zhong Saktimayee Mitra Roy D Martin Watterson

CYP2D6 substrate status is a critical Go/No Go decision criteria in central nervous system (CNS) drug discovery efforts because the polymorphic nature of CYP2D6 can lead to variable patient safety and drug efficacy. In addition, CYP2D6 is disproportionately involved in the metabolism of CNS drugs compared with other drug classes. Therefore, identifying trends in small molecule properties of CNS...

2011
Jean E. Abraham Mel J. Maranian Kristy E. Driver Radka Platte Bolot Kalmyrzaev Caroline Baynes Craig Luccarini Helena M. Earl Alison M. Dunning Carlos Caldas

Background: The gene encoding the phase I enzyme cytochrome P4502D6 (CYP2D6) has been previously investigated for its potential predictive role in the efficacy of breast cancer treatments such as tamoxifen, but its role in breast cancer susceptibility is unclear. This study aims to evaluate the association between germ line variations in CYP2D6 and breast cancer susceptibility. Methods: DNA sam...

2014
Deise C. Friedrich Júlia P. Genro Vinicius A. Sortica Guilherme Suarez-Kurtz Maria Elizabete de Moraes Sergio D. J. Pena Ândrea K. Ribeiro dos Santos Marco A. Romano-Silva Mara H. Hutz Luzia H. Carvalho

The CYP2D6 enzyme is one of the most important members of the cytochrome P450 superfamily. This enzyme metabolizes approximately 25% of currently prescribed medications. The CYP2D6 gene presents a high allele heterogeneity that determines great inter-individual variation. The aim of this study was to evaluate the variability of CYP2D6 alleles, genotypes and predicted phenotypes in Brazilians. E...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2004
Maria Madeira Marc Levine Thomas K H Chang Ahmad Mirfazaelian Gail D Bellward

Clinically, cimetidine therapy impairs the clearance of various drugs metabolized by CYP2D6, such as desipramine and sparteine. Cimetidine is known to reversibly inhibit CYP2D6 in vitro; however, Ki values are greater than plasma concentrations observed in vivo. There is evidence suggesting that this drug may act as an inactivator of cytochrome P450 (P450) enzymes after metabolic activation. Th...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2005
Sharon L Miksys Connie Cheung Frank J Gonzalez Rachel F Tyndale

Polymorphic cytochrome P450 (P450) 2D6 (CYP2D6) metabolizes several classes of therapeutic drugs, endogenous neurochemicals, and toxins. A CYP2D6-humanized transgenic mouse line was previously developed to model CYP2D6-poor and -extensive metabolizer phenotypes. Human CYP2D6 was detected in the liver, kidney, and intestine of these animals. In this study, we investigated further the cellular ex...

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