Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 12, Issue 3, Pages 379-382Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00761-2
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Dihydropyridine 5a was found to be an inhibitor of neuropeptide Y-1 binding in a high throughput I-125-PYY screening assay. Structure-activity studies around certain portions of the dihydropyridine chemotype identified BMS-193885 (6e) as a potent and selective Y-1 receptor antagonist. In a forskolin-stimulated c-AMP production assay using CHO cells expressing the human Y-1 receptor, 6e demonstrated full functional antagonism (K-b = 4.5 nM). Compound 6e inhibited NPY-induced feeding in satiated rats when dosed at 3.0 and 10.0 mg/kg (ip), and also decreased spontaneous overnight food consumption in rats at doses of 10 and 20 mg/kg (ip). (C) 2002 Elsevier Science Ltd. All rights reserved.
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