Literature DB >> 16046122

Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor.

Céline Bonnefous1, Jean-Michel Vernier, John H Hutchinson, Michael F Gardner, Merryl Cramer, Joyce K James, Blake A Rowe, Lorrie P Daggett, Hervé Schaffhauser, Theodore M Kamenecka.   

Abstract

We have identified and synthesized a series of biphenyl-carboxylic acid indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency and the brain to plasma ratio of the initial lead led to the discovery of 5 and 23 (EC50=111 and 5 nM, respectively).

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Year:  2005        PMID： 16046122     DOI： 10.1016/j.bmcl.2005.06.062

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


  15 in total

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Authors:  Douglas J Sheffler; Anthony B Pinkerton; Russell Dahl; Athina Markou; Nicholas D P Cosford
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3.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

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4.  Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.

Authors:  Daniel E O'Brien; Douglas M Shaw; Hyekyung P Cho; Alan J Cross; Steven S Wesolowski; Andrew S Felts; Jonas Bergare; Charles S Elmore; Craig W Lindsley; Colleen M Niswender; P Jeffrey Conn
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Review 5.  Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatment.

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Review 6.  Metabotropic glutamate receptors as therapeutic targets for schizophrenia.

Authors:  Paige N Vinson; P Jeffrey Conn
Journal:  Neuropharmacology       Date:  2011-05-19       Impact factor: 5.250

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

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Journal:  J Med Chem       Date:  2010-12-14       Impact factor: 7.446

8.  The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats.

Authors:  Xinchun Jin; Svetlana Semenova; Li Yang; Robert Ardecky; Douglas J Sheffler; Russell Dahl; P Jeffrey Conn; Nicholas D P Cosford; Athina Markou
Journal:  Neuropsychopharmacology       Date:  2010-06-16       Impact factor: 7.853

9.  Activation of group 2 metabotropic glutamate receptors reduces behavioral and electrographic correlates of pilocarpine induced status epilepticus.

Authors:  Erin H Caulder; Melissa A Riegle; Dwayne W Godwin
Journal:  Epilepsy Res       Date:  2013-11-16       Impact factor: 3.045

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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