Cytochrome P450 3A4-mediated bioactivation of raloxifene: Irreversible enzyme inhibition and thiol adduct formation

Chemical Research in Toxicology

Volumn 15, Issue 7, 2002, Pages 907-914

  Chen, Qing ^a   Ngui, Jason S ^a   Doss, George A ^a   Cai, Xiaoxin ^a   Wang, Regina W ^a   DiNinno, Frank P ^a   Blizzard, Timothy A ^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)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCYSTEINE; CYTOCHROME P450 3A4; GLUTATHIONE; IMMUNOGLOBULIN G; KETOCONAZOLE; RALOXIFENE; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; THIOL; CYP3A PROTEIN, HUMAN; CYTOCHROME P450; ENZYME INHIBITOR; SELECTIVE ESTROGEN RECEPTOR MODULATOR; THIOL DERIVATIVE;

ANIMAL EXPERIMENT; AROMATIZATION; ARTICLE; BILE; CHRONOTHERAPY; CONTROLLED STUDY; DEHYDRATION; DRUG CONJUGATION; DRUG IDENTIFICATION; ENZYME ACTIVITY; ENZYME INACTIVATION; HUMAN; HUMAN CELL; LIQUID CHROMATOGRAPHY; LIVER CELL; LIVER MICROSOME; MALE; MASS SPECTROMETRY; METABOLITE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; OXIDATION; RAT; URINE; ANIMAL; CHEMISTRY; DRUG ANTAGONISM; ENZYMOLOGY; FEMALE; MASS FRAGMENTOGRAPHY; METABOLISM; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; OXIDATION REDUCTION REACTION; SPRAGUE DAWLEY RAT;

ACETYLCYSTEINE; ANIMAL; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME INHIBITORS; FEMALE; GLUTATHIONE; HEPATOCYTES; HUMAN; MAGNETIC RESONANCE SPECTROSCOPY; MALE; MASS FRAGMENTOGRAPHY; MICROSOMES, LIVER; OXIDATION-REDUCTION; RALOXIFENE; RATS; RATS, SPRAGUE-DAWLEY; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SULFHYDRYL COMPOUNDS; ANIMALS; GAS CHROMATOGRAPHY-MASS SPECTROMETRY; HUMANS;

ANIMALIA; ARENE;

EID: 0035996330     PISSN: 0893228X     EISSN: None     Source Type: Journal    
DOI: 10.1021/tx0200109     Document Type: Article

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