2. Academic Validation
  3. Dihydropyridine neuropeptide Y Y(1) receptor antagonists

Dihydropyridine neuropeptide Y Y(1) receptor antagonists

  • Bioorg Med Chem Lett. 2002 Feb 11;12(3):379-82. doi: 10.1016/s0960-894x(01)00761-2.
Graham S Poindexter 1,  Marc A Bruce,  Karen L LeBoulluec,  Ivo Monkovic,  Scott W Martin,  Eric M Parker,  Larry G Iben,  Rachel T McGovern,  Astrid A Ortiz,  Jennifer A Stanley,  Gail K Mattson,  Michael Kozlowski,  Meredith Arcuri,  Ildiko Antal-Zimanyi
Affiliations

Affiliation

  • 1 Pharmaceutical Research Institute, Bristol-Myers Squibb Co., 5 Research Parkway, 06492-7660, Wallingford, CT 06492-7660, USA. graham.poindexter@bms.com
PMID: 11814801 DOI: 10.1016/s0960-894x(01)00761-2
Abstract

Dihydropyridine 5a was found to be an inhibitor of neuropeptide Y(1) binding in a high throughput (125)I-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).

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