Literature DB >> 11814801

Dihydropyridine neuropeptide Y Y(1) receptor antagonists.

Graham S Poindexter1, 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.   

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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Year:  2002        PMID： 11814801     DOI： 10.1016/s0960-894x(01)00761-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  NPY receptors as potential targets for anti-obesity drug development.

Authors:  Ernie Yulyaningsih; Lei Zhang; Herbert Herzog; Amanda Sainsbury
Journal:  Br J Pharmacol       Date:  2011-07       Impact factor: 8.739

2.  Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.

Authors:  Shuanghua Hu; Yazhong Huang; Milind Deshpande; Guanglin Luo; Marc A Bruce; Ling Chen; Gail Mattson; Lawrence G Iben; Jie Zhang; John W Russell; Wendy J Clarke; John B Hogan; Astrid Ortiz; Oliver Flint; Andrew Henwood; Qi Gao; Ildiko Antal-Zimanyi; Graham S Poindexter
Journal:  ACS Med Chem Lett       Date:  2012-01-04       Impact factor: 4.345

Review 3.  PET Imaging of the Neuropeptide Y System: A Systematic Review.

Authors:  Inês C F Fonseca; Miguel Castelo-Branco; Cláudia Cavadas; Antero J Abrunhosa
Journal:  Molecules       Date:  2022-06-09       Impact factor: 4.927

Review 4.  1,4-Dihydropyridines as calcium channel ligands and privileged structures.

Authors:  David J Triggle
Journal:  Cell Mol Neurobiol       Date:  2003-06       Impact factor: 5.046

5.  Structural basis of ligand binding modes at the neuropeptide Y Y1 receptor.

Authors:  Zhenlin Yang; Shuo Han; Max Keller; Anette Kaiser; Brian J Bender; Mathias Bosse; Kerstin Burkert; Lisa M Kögler; David Wifling; Guenther Bernhardt; Nicole Plank; Timo Littmann; Peter Schmidt; Cuiying Yi; Beibei Li; Sheng Ye; Rongguang Zhang; Bo Xu; Dan Larhammar; Raymond C Stevens; Daniel Huster; Jens Meiler; Qiang Zhao; Annette G Beck-Sickinger; Armin Buschauer; Beili Wu
Journal:  Nature       Date:  2018-04-18       Impact factor: 49.962

6.  Spinal Neuropeptide Y1 Receptor-Expressing Neurons Form an Essential Excitatory Pathway for Mechanical Itch.

Authors:  David Acton; Xiangyu Ren; Stefania Di Costanzo; Antoine Dalet; Steeve Bourane; Ilaria Bertocchi; Carola Eva; Martyn Goulding
Journal:  Cell Rep       Date:  2019-07-16       Impact factor: 9.423

7.  Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors.

Authors:  Kazunori Kawamura; Wakana Mori; Masayuki Fujinaga; Tomoteru Yamasaki; Yiding Zhang; Hidekatsu Wakizaka; Akiko Hatori; Lin Xie; Katsushi Kumata; Takayuki Ohkubo; Yusuke Kurihara; Masanao Ogawa; Nobuki Nengaki; Ming-Rong Zhang
Journal:  EJNMMI Radiopharm Chem       Date:  2019-02-18
  7 in total

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