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5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity

Academic Article
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Overview

authors

  • Roppe, J. R.
  • Wang, B. W.
  • Huang, Dee-Hua
  • Tehrani, L.
  • Kamenecka, Theodore
  • Schweiger, E. J.
  • Anderson, J. J.
  • Brodkin, J.
  • Jiang, X. H.
  • Cramer, M.
  • Chung, J.
  • Reyes-Manalo, G.
  • Munoz, B.
  • Cosford, N. D. P.

publication date

  • August 2004

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • Structure-activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo receptor occupancy, and is efficacious in the rat fear-potentiated startle model of anxiety following oral dosing.

subject areas

  • Animals
  • Anti-Anxiety Agents
  • Anxiety
  • Disease Models, Animal
  • Excitatory Amino Acid Antagonists
  • Kinetics
  • Models, Molecular
  • Pyridines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate
  • Structure-Activity Relationship
  • Thiazoles
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Research

keywords

  • MPEP
  • MTEP
  • mGluR
  • mGluR5
  • metabotropic glutamate receptor
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2004.05.037

PubMed ID

  • 15225713
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Additional Document Info

start page

  • 3993

end page

  • 3996

volume

  • 14

issue

  • 15

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