Imidazo[1,2-a]pyridines: Orally Active Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor
Journal of Medicinal Chemistry2012Vol. 55(6), pp. 2688–2701
Citations Over TimeTop 10% of 2012 papers
Andrés A. Trabanco, Gary Tresadern, Gregor J. Macdonald, Juan A. Vega, Ana Isabel de Lucas, Encarnación Matesanz, Aránzazu García, María Lourdes Linares, Sergio A. Alonso de Diego, José Manuel Alonso Segura, Daniel Oehlrich, A. Ahnaou, Wilhelmus Drinkenburg, Claire Mackie, José Ignacio Andrés, Hilde Lavreysen, José M. Cid
Abstract
Advanced leads of an imidazopyridine series of positive allosteric modulators of the metabotropic glutamate 2 (mGlu2) receptor are reported. The optimization of in vitro ADMET and in vivo pharmacokinetic properties led to the identification of 27o. With good potency and selectivity for the mGlu2 receptor, 27o affected sleep-wake architecture in rats after oral treatment, which we have previously shown to be indicative of mGlu2 receptor-mediated central activity.
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