Literature DB >> 20638279

An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.

Stephen P East1, Samantha Bamford, Matthias G A Dietz, Christian Eickmeier, Adam Flegg, Boris Ferger, Mark J Gemkow, Ralf Heilker, Bastian Hengerer, Adrian Kotey, Pui Loke, Gerhard Schänzle, Hans-Dieter Schubert, John Scott, Mark Whittaker, Mildred Williams, Przemyslaw Zawadzki, Kai Gerlach.   

Abstract

A high-throughput screening campaign identified 4-((E)-styryl)-pyrimidin-2-ylamine (11) as a positive allosteric modulator of the metabotropic glutamate (mGlu) receptor subtype 4. An evaluation of the structure-activity relationships (SAR) of 11 is described and the efficacy of this compound in a haloperidol-induced catalepsy rat model following oral administration is presented. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20638279     DOI： 10.1016/j.bmcl.2010.06.078

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


  17 in total

1.  Allosteric modulation of the group III mGlu4 receptor provides functional neuroprotection in the 6-hydroxydopamine rat model of Parkinson's disease.

Authors:  Matthew J Betts; Michael J O'Neill; Susan Duty
Journal:  Br J Pharmacol       Date:  2012-08       Impact factor: 8.739

2.  Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.

Authors:  Carrie K Jones; Darren W Engers; Analisa D Thompson; Julie R Field; Anna L Blobaum; Stacey R Lindsley; Ya Zhou; Rocco D Gogliotti; Satyawan Jadhav; Rocio Zamorano; Jim Bogenpohl; Yoland Smith; Ryan Morrison; J Scott Daniels; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  J Med Chem       Date:  2011-10-19       Impact factor: 7.446

3.  The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia.

Authors:  Ranjani Ponnazhagan; Ashley S Harms; Aaron D Thome; Asta Jurkuvenaite; Rocco Gogliotti; Colleen M Niswender; P Jeffrey Conn; David G Standaert
Journal:  J Neuroimmune Pharmacol       Date:  2016-02-12       Impact factor: 4.147

Review 4.  Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.

Authors:  Albert J Robichaud; Darren W Engers; Craig W Lindsley; Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2011-06-14       Impact factor: 4.418

Review 5.  Development of allosteric modulators of GPCRs for treatment of CNS disorders.

Authors:  Hilary Highfield Nickols; P Jeffrey Conn
Journal:  Neurobiol Dis       Date:  2013-09-27       Impact factor: 5.996

6.  The metabotropic glutamate receptor 8 agonist (S)-3,4-DCPG reverses motor deficits in prolonged but not acute models of Parkinson's disease.

Authors:  Kari A Johnson; Carrie K Jones; Mohammed N Tantawy; Michael Bubser; Marketa Marvanova; M Sib Ansari; Ronald M Baldwin; P Jeffrey Conn; Colleen M Niswender
Journal:  Neuropharmacology       Date:  2012-04-21       Impact factor: 5.250

7.  Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.

Authors:  Darren W Engers; Julie R Field; Uyen Le; Ya Zhou; Julie D Bolinger; Rocio Zamorano; Anna L Blobaum; Carrie K Jones; Satyawan Jadhav; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  J Med Chem       Date:  2011-01-19       Impact factor: 7.446

8.  The antipsychotic-like effects of positive allosteric modulators of metabotropic glutamate mGlu4 receptors in rodents.

Authors:  Anna Sławińska; Joanna M Wierońska; Katarzyna Stachowicz; Marcin Marciniak; Magdalena Lasoń-Tyburkiewicz; Piotr Gruca; Mariusz Papp; Magdalena Kusek; Krzysztof Tokarski; Darío Doller; Andrzej Pilc
Journal:  Br J Pharmacol       Date:  2013-08       Impact factor: 8.739

9.  Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.

Authors:  Colleen M Niswender; Carrie K Jones; Xin Lin; Michael Bubser; Analisa Thompson Gray; Anna L Blobaum; Darren W Engers; Alice L Rodriguez; Matthew T Loch; J Scott Daniels; Craig W Lindsley; Corey R Hopkins; Jonathan A Javitch; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2016-08-05       Impact factor: 4.418

Review 10.  Recent advances in the medicinal chemistry of group II and group III mGlu receptors.

Authors:  Chaobin Jin; Shutao Ma
Journal:  Medchemcomm       Date:  2017-01-13       Impact factor: 3.597
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