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 ,
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
