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

Bioorganic & Medicinal Chemistry Letters
Jeffrey RoppeNicholas D P Cosford

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.

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Citations

Aug 12, 2009·The Journal of Pharmacology and Experimental Therapeutics·Liyun WangStuart Maudsley
Sep 1, 2015·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Robert W GouldCarrie K Jones
Nov 3, 2010·Neuropharmacology·F NicolettiJ P Pin
Mar 18, 2008·Current Opinion in Chemical Biology·Jana A LewisCraig W Lindsley
Jun 22, 2007·Pharmacology & Therapeutics·Agnieszka Palucha, Andrzej Pilc
Sep 24, 2005·Basic & Clinical Pharmacology & Toxicology·Andreas RitzénChristian Thomsen
Dec 17, 2009·Angewandte Chemie·Nicholas A Afagh, Andrei K Yudin
Jun 29, 2006·The Journal of Pharmacology and Experimental Therapeutics·Xia LiJeffrey M Witkin
Apr 30, 2008·Journal of Chemical Information and Modeling·Sebastian RadestockSteffen Renner
Sep 6, 2018·Journal of Medicinal Chemistry·Mingcheng QianSerge Van Calenbergh

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