Comparative Biotransformation of Pyrazinone-containing Corticotropin-releasing Factor Receptor-1 (crf-r1) Antagonists: Minimizing the Reactive Metabolite Formation
نویسندگان
چکیده
XIAOLIANG ZHUO, RICHARD A. HARTZ, JOANNE J. BRONSON, HARVEY WONG*, VIJAY T. AHUJA, VIVEKANANDA M. VRUDHULA, JOHN E. LEET, STELLA HUANG, JOHN E. MACOR, YUE-ZHONG SHU Department of Biotransformation (X.Z., Y.-Z.S.), Neuroscience Chemistry (R.A.H., J.J.B., V.T.A., V.M.V., J.E.M.), Discovery Metabolism and Pharmacokinetics (H.W.), Discovery Analytical Sciences (S.H.), Synthesis & Analysis Technology (J.E.L.), BristolMyers Squibb Co., 5 Research Parkway, Wallingford, CT 06492 DMD Fast Forward. Published on October 15, 2009 as doi:10.1124/dmd.109.028910
منابع مشابه
Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation.
(S)-5-Chloro-1-(1-cyclopropylethyl)-3-(2,6-dichloro-4-(trifluoromethyl)phenylamino)pyrazin-2(1H)-one (BMS-665053), a pyrazinone-containing compound, is a potent and selective antagonist of corticotropin-releasing factor receptor-1 (CRF-R1) that showed efficacy in the defensive withdrawal model for anxiety in rats, suggesting its use as a potential treatment for anxiety and depression. In vitro ...
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