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Kjell Fuxe, Dasiel O Borroto-Escuela
INTRODUCTION: Metabotropic glutamate receptor 5 (mGlu5) negative allosteric modulators (NAM) such as 2-Methyl-6-(phenylethynyl)pyridine (MPEP) and 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine (MTEP) can produce antidepressant-like effects; an example being the forced swim test in rodents. It is therefore of high interest that a new mGlu5 NAM called basimglurant (RO4917523, RG7090) was recently introduced for clinical development in depression. AREAS COVERED: The current article reports on the preclinical and clinical work with basimglurant which strongly supports its use for treatment of depression...
2015: Expert Opinion on Investigational Drugs
Lothar Lindemann, Richard H Porter, Sebastian H Scharf, Basil Kuennecke, Andreas Bruns, Markus von Kienlin, Anthony C Harrison, Axel Paehler, Christoph Funk, Andreas Gloge, Manfred Schneider, Neil J Parrott, Liudmila Polonchuk, Urs Niederhauser, Stephen R Morairty, Thomas S Kilduff, Eric Vieira, Sabine Kolczewski, Juergen Wichmann, Thomas Hartung, Michael Honer, Edilio Borroni, Jean-Luc Moreau, Eric Prinssen, Will Spooren, Joseph G Wettstein, Georg Jaeschke
Major depressive disorder (MDD) is a serious public health burden and a leading cause of disability. Its pharmacotherapy is currently limited to modulators of monoamine neurotransmitters and second-generation antipsychotics. Recently, glutamatergic approaches for the treatment of MDD have increasingly received attention, and preclinical research suggests that metabotropic glutamate receptor 5 (mGlu5) inhibitors have antidepressant-like properties. Basimglurant (2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine) is a novel mGlu5 negative allosteric modulator currently in phase 2 clinical development for MDD and fragile X syndrome...
April 2015: Journal of Pharmacology and Experimental Therapeutics
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