کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366947 981611 2007 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites
چکیده انگلیسی

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).

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 protein modification was assessed and was found to be acceptable (<50 pmol-equiv/mg protein).Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 2, 15 January 2007, Pages 301–304
نویسندگان
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