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Improved Detection of Reactive Metabolites with a Bromine‐containing Glutathione Analog Using Mass Defect and Isotope Pattern Matching by André LeBlanc; Tze Chieh Shiao; René Roy; Lekha Sleno is a Chemistry article available to read on EtoBox.

What is Improved Detection of Reactive Metabolites with a Bromine‐containing Glutathione Analog Using Mass Defect and Isotope Pattern Matching about?

## Abstract Drug bioactivation leading to the formation of reactive species capable of covalent binding to proteins represents an important cause of drug‐induced toxicity. Reactive metabolite detection using __in__ __vitro__ microsomal incubations is a crucial step in assessing potential toxicity of pharmaceutical compounds. The most common method for screening the formation of these unstable, electrophilic species is by trapping them with glutathione (GSH) followed by liquid chromatography/mass spectrometry (LC/MS) analysis. The present work describes the use of a brominated analog of glutathione, __N__‐(2‐bromocarbobenzyloxy)‐GSH (GSH‐Br), for the __in__ __vitro__ screening of reactive metabolites by LC/MS. This novel trapping agent was tested with four drug compounds known to form reactive metabolites, acetaminophen, fipexide, trimethoprim and clozapine. __In__ __vitro__ rat microsomal incubations were performed with GSH and GSH‐Br for each drug with subsequent analysis by liquid chromatography/high‐resolution mass spectrometry on an electrospray time‐of‐flight (ESI‐TOF) instrument. A generic LC/MS method was used for data acquisition, followed by drug‐specific processing of acc

Who reads Improved Detection of Reactive Metabolites with a Bromine‐containing Glutathione Analog Using Mass Defect and Isotope Pattern Matching?

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Author
André LeBlanc; Tze Chieh Shiao; René Roy; Lekha Sleno
Publisher
John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0951-4198)
Published
2010
Language
EN
Field
Chemistry (Physical Sciences)

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