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The identification of structurally novel,selective, orally bioavailable positive modulators of mGluR2 |
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| Authors: | Pier L. D’Alessandro Corrado Corti Adelheid Roth Annarosa Ugolini Anna Sava Dino Montanari Federica Bianchi Stephen L. Garland Ben Powney Emma L. Koppe Magalie Rocheville Greg Osborne Paloma Perez Jesús de la Fuente Maite De Los Frailes Paul W. Smith Clive Branch David Nash Stephen P. Watson |
| Affiliation: | 1. GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK;2. GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicines Research Centre, Verona, Italy;3. GlaxoSmithKline, Molecular Discovery Research, New Frontiers Science Park, Harlow, UK;4. GlaxoSmithKline, Molecular Discovery Research, Tres Cantos, Madrid, Spain |
| Abstract: | The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure–activity relationships, attenuation of dopaminergic activity, and potentiation of mGluR2 responses in rat hippocampal MPP-DG synapses are also reported. |
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