Literature DB >> 22267125

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.

Ralf Mueller1, 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.   

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Year:  2012        PMID： 22267125      PMCID： PMC3517057          DOI： 10.1002/cmdc.201100510

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


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  44 in total

1.  Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice.

Authors:  C Chiamulera; M P Epping-Jordan; A Zocchi; C Marcon; C Cottiny; S Tacconi; M Corsi; F Orzi; F Conquet
Journal:  Nat Neurosci       Date:  2001-09       Impact factor: 24.884

Review 2.  Modulation of the basal ganglia by metabotropic glutamate receptors: potential for novel therapeutics.

Authors:  Michael J Marino; P Jeffrey Conn; Jeffrey P Conn
Journal:  Curr Drug Targets CNS Neurol Disord       Date:  2002-06

Review 3.  Direct and indirect modulation of the N-methyl D-aspartate receptor.

Authors:  M J Marino; P Jeffrey Conn
Journal:  Curr Drug Targets CNS Neurol Disord       Date:  2002-02

Review 4.  mGluR5 antagonists: discovery, characterization and drug development.

Authors:  Fabrizio Gasparini; Graeme Bilbe; Baltazar Gomez-Mancilla; Will Spooren
Journal:  Curr Opin Drug Discov Devel       Date:  2008-09

5.  3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.

Authors:  Andrew S Felts; Stacey R Lindsley; Jeffrey P Lamb; Alice L Rodriguez; Usha N Menon; Satyawan Jadhav; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2010-06-15       Impact factor: 2.823

6.  Major tranquillizers can be distinguished from minor tranquillizers on the basis of effects on marble burying and swim-induced grooming in mice.

Authors:  C L Broekkamp; H W Rijk; D Joly-Gelouin; K L Lloyd
Journal:  Eur J Pharmacol       Date:  1986-07-31       Impact factor: 4.432

7.  Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes.

Authors:  Yongqin Zhang; Alice L Rodriguez; P Jeffrey Conn
Journal:  J Pharmacol Exp Ther       Date:  2005-08-31       Impact factor: 4.030

Review 8.  Metabotropic glutamate receptors as novel targets for anxiety and stress disorders.

Authors:  Chad J Swanson; Mark Bures; Michael P Johnson; Anni-Maija Linden; James A Monn; Darryle D Schoepp
Journal:  Nat Rev Drug Discov       Date:  2005-02       Impact factor: 84.694

9.  Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents.

Authors:  Gene G Kinney; Maryann Burno; Una C Campbell; Lisa M Hernandez; Dana Rodriguez; Linda J Bristow; P Jeffrey Conn
Journal:  J Pharmacol Exp Ther       Date:  2003-03-26       Impact factor: 4.030

Review 10.  Metabotropic glutamate receptors: physiology, pharmacology, and disease.

Authors:  Colleen M Niswender; P Jeffrey Conn
Journal:  Annu Rev Pharmacol Toxicol       Date:  2010       Impact factor: 13.820
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  21 in total

1.  Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding.

Authors:  Mariusz Butkiewicz; Alice L Rodriguez; Shane E Rainey; Joshua Wieting; Vincent B Luscombe; Shaun R Stauffer; Craig W Lindsley; P Jeffrey Conn; Jens Meiler
Journal:  ACS Chem Neurosci       Date:  2019-06-17       Impact factor: 4.418

Review 2.  Computational methods in drug discovery.

Authors:  Gregory Sliwoski; Sandeepkumar Kothiwale; Jens Meiler; Edward W Lowe
Journal:  Pharmacol Rev       Date:  2013-12-31       Impact factor: 25.468

3.  Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology.

Authors:  Kathy Sengmany; Shane D Hellyer; Sabine Albold; Taide Wang; P Jeffrey Conn; Lauren T May; Arthur Christopoulos; Katie Leach; Karen J Gregory
Journal:  Neuropharmacology       Date:  2019-02-11       Impact factor: 5.250

4.  Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.

Authors:  Karen J Gregory; Elizabeth D Nguyen; Chrysa Malosh; Jeffrey L Mendenhall; Jessica Z Zic; Brittney S Bates; Meredith J Noetzel; Emma F Squire; Eric M Turner; Jerri M Rook; Kyle A Emmitte; Shaun R Stauffer; Craig W Lindsley; Jens Meiler; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2014-02-26       Impact factor: 4.418

Review 5.  In Silico Studies in Drug Research Against Neurodegenerative Diseases.

Authors:  Farahnaz Rezaei Makhouri; Jahan B Ghasemi
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

6.  N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.

Authors:  Andrew S Felts; Alice L Rodriguez; Ryan D Morrison; Daryl F Venable; Anna L Blobaum; Frank W Byers; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2016-03-09       Impact factor: 2.823

7.  Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Authors:  Andrew S Felts; Alice L Rodriguez; Ryan D Morrison; Daryl F Venable; Jason T Manka; Brittney S Bates; Anna L Blobaum; Frank W Byers; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2013-09-10       Impact factor: 2.823

8.  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

9.  Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.

Authors:  Russell J Amato; Andrew S Felts; Alice L Rodriguez; Daryl F Venable; Ryan D Morrison; Frank W Byers; J Scott Daniels; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Carrie K Jones; Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2013-05-29       Impact factor: 4.418

10.  Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.

Authors:  Alexander R Geanes; Hykeyung P Cho; Kellie D Nance; Kevin M McGowan; P Jeffrey Conn; Carrie K Jones; Jens Meiler; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2016-07-30       Impact factor: 2.823
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