Interaction of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 with the Negative Allosteric Antagonist Site Is Required for Potentiation of Receptor Responses

Yelin Chen; Yi Nong; Cyril Goudet; Kamondanai Hemstapat; Tomas de Paulis; Jean-Philippe Pin; P. Jeffrey Conn

doi:10.1124/mol.106.032425

Interaction of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 with the Negative Allosteric Antagonist Site Is Required for Potentiation of Receptor Responses

Molecular Pharmacology ◽

10.1124/mol.106.032425 ◽

2007 ◽

Vol 71 (5) ◽

pp. 1389-1398 ◽

Cited By ~ 71

Author(s):

Yelin Chen ◽

Yi Nong ◽

Cyril Goudet ◽

Kamondanai Hemstapat ◽

Tomas de Paulis ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2015.10.050 ◽

2015 ◽

Vol 25 (24) ◽

pp. 5792-5796 ◽

Cited By ~ 5

Author(s):

John M. Ellard ◽

Andrew Madin ◽

Oliver Philps ◽

Mark Hopkin ◽

Scott Henderson ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Preclinical Model ◽

Allosteric Modulators ◽

Improve Performance ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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N-Aryl Piperazine Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators Possess Efficacy in Preclinical Models of NMDA Hypofunction and Cognitive Enhancement

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.113.206623 ◽

2013 ◽

Vol 347 (2) ◽

pp. 438-457 ◽

Cited By ~ 34

Author(s):

K.J. Gregory ◽

E.J. Herman ◽

A.J. Ramsey ◽

A.S. Hammond ◽

N.E. Byun ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Cognitive Enhancement ◽

Allosteric Modulators ◽

Preclinical Models ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators

ACS Medicinal Chemistry Letters ◽

10.1021/acsmedchemlett.6b00292 ◽

2016 ◽

Vol 7 (12) ◽

pp. 1082-1086 ◽

Cited By ~ 12

Author(s):

Matthew D. Hill ◽

Haiquan Fang ◽

Jeffrey M. Brown ◽

Thaddeus Molski ◽

Amy Easton ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Metabotropic glutamate receptor 5 positive allosteric modulators are neuroprotective in a mouse model of H untington's disease

British Journal of Pharmacology ◽

10.1111/bph.12164 ◽

2013 ◽

Vol 169 (4) ◽

pp. 909-921 ◽

Cited By ~ 45

Author(s):

JG Doria ◽

FR Silva ◽

JM Souza ◽

LB Vieira ◽

TG Carvalho ◽

...

Keyword(s):

Mouse Model ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias

Molecular Pharmacology ◽

10.1124/molpharm.120.000185 ◽

2021 ◽

Vol 99 (5) ◽

pp. 328-341

Author(s):

Angela Arsova ◽

Thor C. Møller ◽

Shane D. Hellyer ◽

Line Vedel ◽

Simon R. Foster ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004–2012)

Pharmaceutical Patent Analyst ◽

10.4155/ppa.12.82 ◽

2013 ◽

Vol 2 (1) ◽

pp. 93-108 ◽

Cited By ~ 20

Author(s):

Craig W Lindsley ◽

Shaun R Stauffer

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2014.04.087 ◽

2014 ◽

Vol 24 (15) ◽

pp. 3641-3646 ◽

Cited By ~ 4

Author(s):

Mark Turlington ◽

Meredith J. Noetzel ◽

Thomas M. Bridges ◽

Paige N. Vinson ◽

Thomas Steckler ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Ligand Efficiency ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators ◽

High Ligand

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Metabotropic glutamate receptor 5 (mGlu 5 )‐positive allosteric modulators differentially induce or potentiate desensitization of mGlu 5 signaling in recombinant cells and neurons

Journal of Neurochemistry ◽

10.1111/jnc.14844 ◽

2019 ◽

Vol 151 (3) ◽

pp. 301-315 ◽

Cited By ~ 2

Author(s):

Shane D. Hellyer ◽

Sabine Albold ◽

Kathy Sengmany ◽

Junaid Singh ◽

Katie Leach ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Recombinant Cells ◽

Positive Allosteric Modulators

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Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2015.01.038 ◽

2015 ◽

Vol 25 (6) ◽

pp. 1310-1317 ◽

Cited By ~ 7

Author(s):

María Luz Martín-Martín ◽

José Manuel Bartolomé-Nebreda ◽

Susana Conde-Ceide ◽

Sergio A. Alonso de Diego ◽

Silvia López ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2011.01.027 ◽

2011 ◽

Vol 21 (5) ◽

pp. 1402-1406 ◽

Cited By ~ 23

Author(s):

Jeffrey G. Varnes ◽

Andrew P. Marcus ◽

Russell C. Mauger ◽

Scott R. Throner ◽

Valerie Hoesch ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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