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
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