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.

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

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

Affiliation

Zhang Z; Department of Drug Metabolism, Merck Research Laboratories, Rahway, New Jersey 07065, USA. zhoupen_zhang@merck.com

Chem Res Toxicol ; 18(4): 675-85, 2005 Apr.

Article in En | MEDLINE | ID: mdl-15833027

Subject(s)

Cytochrome P-450 Enzyme System/physiology; Microsomes, Liver/metabolism; Oxathiins/pharmacokinetics; Selective Estrogen Receptor Modulators/pharmacokinetics; Benzoquinones/metabolism; Biotransformation; Cytochrome P-450 CYP3A; Hepatocytes/metabolism; Humans; Magnetic Resonance Spectroscopy; Mass Spectrometry; Protein Binding

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Collection: 01-internacional Database: MEDLINE Main subject: Oxathiins / Microsomes, Liver / Selective Estrogen Receptor Modulators / Cytochrome P-450 Enzyme System Limits: Humans Language: En Journal: Chem Res Toxicol Journal subject: TOXICOLOGIA Year: 2005 Document type: Article Affiliation country: United States Country of publication: United States

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