• Title of article

    In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites

  • Author/Authors

    Deborah A. Nicoll-Griffith، نويسنده , , Carmai Seto، نويسنده , , Yves Aubin، نويسنده , , Jean François Lévesque، نويسنده , , Nathalie Chauret، نويسنده , , Stephen Day، نويسنده , , Jose M. Silva، نويسنده , , Laird A. Trimble، نويسنده , , Jean François Truchon، نويسنده , , Carl Berthelette، نويسنده , , Nicolas Lachance، نويسنده , , Zhaoyin Wang، نويسنده , , Claudio Sturino، نويسنده , , Matt Braun، نويسنده , , Robert Zamboni، نويسنده , , Robert N. Young، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2007
  • Pages
    4
  • From page
    301
  • To page
    304
  • Abstract
    Metabolites of the potent DP antagonist, MK-0524, were generated using in vitro systems including hepatic microsomes and hepatocytes. Four metabolites (two hydroxylated diastereomers, a ketone and an acyl glucuronide) were characterized by LC–MS/MS and 1H NMR. Larger quantities of these metabolites were prepared by either organic synthesis or biosynthetically to be used as standards in other studies. The propensity for covalent binding was assessed and was found to be acceptable (<50 pmol-equiv/mg protein).
  • Keywords
    DP receptor antagonist , MK-0524 , Biotransformations , metabolites , Reactive intermediates
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2007
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    797643