Literature DB >> 12565928

[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.

Nicholas D P Cosford1, Jeffrey Roppe, Lida Tehrani, Edwin J Schweiger, T Jon Seiders, Ashok Chaudary, Sara Rao, Mark A Varney.   

Abstract

The design, synthesis, and characterization of two potent, non-competitive radioligands, [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy, that are selective for the mGlu5 receptor are described.

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Year:  2003        PMID： 12565928     DOI： 10.1016/s0960-894x(02)00997-6

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


  40 in total

1.  Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.

Authors:  Alice L Rodriguez; Mark D Grier; Carrie K Jones; Elizabeth J Herman; Alexander S Kane; Randy L Smith; Richard Williams; Ya Zhou; Joy E Marlo; Emily L Days; Tasha N Blatt; Satyawan Jadhav; Usha N Menon; Paige N Vinson; Jerri M Rook; Shaun R Stauffer; Colleen M Niswender; Craig W Lindsley; C David Weaver; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2010-10-05       Impact factor: 4.436

2.  In vivo positron emission tomography imaging with [¹¹C]ABP688: binding variability and specificity for the metabotropic glutamate receptor subtype 5 in baboons.

Authors:  Christine DeLorenzo; Matthew S Milak; Kathleen G Brennan; J S Dileep Kumar; J John Mann; Ramin V Parsey
Journal:  Eur J Nucl Med Mol Imaging       Date:  2011-01-29       Impact factor: 9.236

3.  Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.

Authors:  Ralf Mueller; Eric S Dawson; Jens Meiler; Alice L Rodriguez; Brian A Chauder; Brittney S Bates; Andrew S Felts; Jeffrey P Lamb; Usha N Menon; Sataywan B Jadhav; Alexander S Kane; Carrie K Jones; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn; Christopher M Olsen; Danny G Winder; Kyle A Emmitte; Craig W Lindsley
Journal:  ChemMedChem       Date:  2012-01-20       Impact factor: 3.466

4.  Interaction of blockers of ionotropic NMDA receptors and metabotropic glutamate receptors in a working memory test in rats.

Authors:  Y A Novitskaya; O A Dravolina; E E Zvartau; W Danysz; A Y Bespalov
Journal:  Neurosci Behav Physiol       Date:  2010-07-17

Review 5.  Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Authors:  Craig W Lindsley; Kyle A Emmitte; Corey R Hopkins; Thomas M Bridges; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn
Journal:  Chem Rev       Date:  2016-02-16       Impact factor: 60.622

Review 6.  Ionotropic and metabotropic glutamate receptor structure and pharmacology.

Authors:  James N C Kew; John A Kemp
Journal:  Psychopharmacology (Berl)       Date:  2005-02-25       Impact factor: 4.530

7.  Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation.

Authors:  Karen J Gregory; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2015-03-25       Impact factor: 4.436

8.  Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.

Authors:  Alexis S Hammond; Alice L Rodriguez; Steven D Townsend; Colleen M Niswender; Karen J Gregory; Craig W Lindsley; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2010-08-19       Impact factor: 4.418

9.  The role of ventral and dorsal striatum mGluR5 in relapse to cocaine-seeking and extinction learning.

Authors:  Lori A Knackstedt; Heather L Trantham-Davidson; Marek Schwendt
Journal:  Addict Biol       Date:  2013-05-27       Impact factor: 4.280

10.  Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Authors:  Brittney S Bates; Alice L Rodriguez; Andrew S Felts; Ryan D Morrison; Daryl F Venable; Anna L Blobaum; Frank W Byers; Kera P Lawson; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2014-06-11       Impact factor: 2.823
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