2. Academic Validation
  3. The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2

The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2

  • Bioorg Med Chem Lett. 2010 Jan 15;20(2):759-62. doi: 10.1016/j.bmcl.2009.11.032.
Pier L D'Alessandro 1,  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
Affiliations

Affiliation

  • 1 GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
PMID: 20005096 DOI: 10.1016/j.bmcl.2009.11.032
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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