Literature DB >> 20005096

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

Pier L D'Alessandro1, 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.   

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. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20005096     DOI： 10.1016/j.bmcl.2009.11.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Authors:  Bruce J Melancon; Corey R Hopkins; Michael R Wood; Kyle A Emmitte; Colleen M Niswender; Arthur Christopoulos; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2012-01-06       Impact factor: 7.446

Review 2.  Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

Authors:  Douglas J Sheffler; Anthony B Pinkerton; Russell Dahl; Athina Markou; Nicholas D P Cosford
Journal:  ACS Chem Neurosci       Date:  2011-04-12       Impact factor: 4.418

3.  Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

Authors:  Raveendra-Panickar Dhanya; Shyama Sidique; Douglas J Sheffler; Hilary Highfield Nickols; Ananda Herath; Li Yang; Russell Dahl; Robert Ardecky; Svetlana Semenova; Athina Markou; P Jeffrey Conn; Nicholas D P Cosford
Journal:  J Med Chem       Date:  2010-12-14       Impact factor: 7.446

Review 4.  Therapeutic potential of targeting glutamate receptors in Parkinson's disease.

Authors:  Clare Finlay; Susan Duty
Journal:  J Neural Transm (Vienna)       Date:  2014-02-21       Impact factor: 3.575

Review 5.  Targeting glutamate receptors to tackle the pathogenesis, clinical symptoms and levodopa-induced dyskinesia associated with Parkinson's disease.

Authors:  Susan Duty
Journal:  CNS Drugs       Date:  2012-12       Impact factor: 5.749

6.  Discovery of a small molecule targeting SET-PP2A interaction to overcome BCR-ABLT315I mutation of chronic myeloid leukemia.

Authors:  Shuzhen Wang; Weiquan Xie; Duowei Wang; Zhigang Peng; Yan Zheng; Nan Liu; Wen Dai; Yang Wang; Zongqiang Wang; Yong Yang; Yijun Chen
Journal:  Oncotarget       Date:  2015-05-20
  6 in total

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