Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

F. Gasparini, Kurt Lingenhöhl, Natacha Stoehr et al. · Neuropharmacology · 1999 · 720 citations

Medicine, Medicinal Chemistry, Pharmacology +7

Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of <i>N</i>-(1,3-Diphenyl-1<i>H</i>- pyrazol-5-yl)benzamides That Potentiate Receptor Function in Vivo

Craig W. Lindsley, David D. Wisnoski, William Leister et al. · Journal of Medicinal Chemistry · 2004 · 171 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +17

A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators

Alice L. Rodriguez, Yi Nong, Nishant K. Sekaran et al. · Molecular Pharmacology · 2005 · 125 citations

Medicine, Neuroscience, Pharmacology +17

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

Sameer Sharma, Alice L. Rodriguez, P. Jeffrey Conn et al. · Bioorganic & Medicinal Chemistry Letters · 2008 · 84 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17

Discovery of a Novel Chemical Class of mGlu₅ Allosteric Ligands with Distinct Modes of Pharmacology

Alexis S. Hammond, Alice L. Rodriguez, Steven D. Townsend et al. · ACS Chemical Neuroscience · 2010 · 73 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +17