Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold
- 15 July 2008
- journal article
- research article
- Published by Elsevier in Bioorganic & Medicinal Chemistry Letters
- Vol. 18 (14) , 4098-4101
- https://doi.org/10.1016/j.bmcl.2008.05.091
Abstract
No abstract availableKeywords
This publication has 15 references indexed in Scilit:
- Application of Combinatorial Chemistry Science on Modern Drug DiscoveryJournal of Combinatorial Chemistry, 2008
- Metabotropic Glutamate Receptor Subtype 5 Antagonists MPEP and MTEPCNS Drug Reviews, 2006
- Substituent Effects ofN-(1,3-Diphenyl-1H-pyrazol-5-yl)benzamides on Positive Allosteric Modulation of the Metabotropic Glutamate-5 Receptor in Rat Cortical AstrocytesJournal of Medicinal Chemistry, 2006
- 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 ModulatorsMolecular Pharmacology, 2005
- Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist ActivityThe Journal of Pharmacology and Experimental Therapeutics, 2005
- A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral ModelsThe Journal of Pharmacology and Experimental Therapeutics, 2005
- Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That Potentiate Receptor Function in VivoJournal of Medicinal Chemistry, 2004
- 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 activityBioorganic & Medicinal Chemistry Letters, 2004
- A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat ForebrainThe Journal of Pharmacology and Experimental Therapeutics, 2004
- PHARMACOLOGY AND FUNCTIONS OF METABOTROPIC GLUTAMATE RECEPTORSAnnual Review of Pharmacology and Toxicology, 1997