In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: Formation of reactive iminium and quinone type metabolites

Chemical Research in Toxicology

Volumn 18, Issue 4, 2005, Pages 675-685

  Zhang, Zhoupeng ^a   Chen, Qing ^a   Li, Ying ^a   Doss, George A ^a   Dean, Brian J ^a   Ngui, Jason S ^a   Elipe, Maria Silva ^a,b   Kim, Seongkon ^a   Wu, Jane Y ^a   DiNinno, Frank ^a   Hammond, Milton L ^a   Stearns, Ralph A ^a   Evans, David C ^a   Baillie, Thomas A ^a   Tang, Wei ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (3 HYDROXYPHENYL) 2 [4 (2 PYRROLIDIN 1 YLETHOXY)PHENYL] 2,3 DIHYDRO 1,4 BENZOXATHIIN 6 OL; 3 (4 HYDROXYPHENYL) 2 [4 (2 PIPERIDIN 1 YLETHOXY)PHENYL] 2,3 DIHYDRO 1,4 BENZOXATHIIN 6 OL; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; DIHYDROBENZOXATHIIN DERIVATIVE; ESTROGEN RECEPTOR ALPHA; IMMUNOGLOBULIN G ANTIBODY; KETOCONAZOLE; QUINIDINE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TRITIUM; UNCLASSIFIED DRUG;

ARTICLE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN TISSUE; IN VITRO STUDY; LIQUID CHROMATOGRAPHY; LIVER MICROSOME; MASS SPECTROMETRY; METABOLITE; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; OXIDATION REDUCTION REACTION; POLYACRYLAMIDE GEL ELECTROPHORESIS; POSTMENOPAUSE; POSTMENOPAUSE OSTEOPOROSIS; PROTEIN BINDING; RADIOACTIVITY;

BENZOQUINONES; BIOTRANSFORMATION; CYTOCHROME P-450 ENZYME SYSTEM; HEPATOCYTES; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MASS SPECTROMETRY; MICROSOMES, LIVER; OXATHIINS; PROTEIN BINDING; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 20244376331     PISSN: 0893228X     EISSN: None     Source Type: Journal    
DOI: 10.1021/tx0496789     Document Type: Article

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