A double effect molecular switch leads to a novel potent negative allosteric modulator of metabotropic glutamate receptor 5

Double Effect ◽

Molecular Switch ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a “Molecular Switch” in PAM Pharmacology

Molecular Pharmacology ◽

10.1124/mol.112.083949 ◽

2013 ◽

Vol 83 (5) ◽

pp. 991-1006 ◽

Cited By ~ 60

Author(s):

Karen J. Gregory ◽

Elizabeth D. Nguyen ◽

Sean D. Reiff ◽

Emma F. Squire ◽

Shaun R. Stauffer ◽

...

Keyword(s):

Glutamate Receptor ◽

Point Mutations ◽

Binding Pocket ◽

Molecular Switch ◽

Allosteric Modulator ◽

Positive Allosteric Modulator ◽

Metabotropic Glutamate

Attenuation of reinstatement of methamphetamine-, sucrose-, and food-seeking behavior in rats by fenobam, a metabotropic glutamate receptor 5 negative allosteric modulator

Psychopharmacology ◽

10.1007/s00213-012-2804-z ◽

2012 ◽

Vol 225 (1) ◽

pp. 151-159 ◽

Cited By ~ 23

Author(s):

Lucas R. Watterson ◽

Peter R. Kufahl ◽

Natali E. Nemirovsky ◽

Kaveish Sewalia ◽

Lauren E. Hood ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

Seeking Behavior ◽

Negative Allosteric Modulator ◽

Food Seeking

The metabotropic glutamate receptor 5 negative allosteric modulator fenobam

Pain ◽

10.1097/j.pain.0000000000001695 ◽

2020 ◽

Vol 161 (1) ◽

pp. 135-146 ◽

Cited By ~ 1

Author(s):

Laura F. Cavallone ◽

Michael C. Montana ◽

Karen Frey ◽

Dorina Kallogjeri ◽

James M. Wages ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

Basimglurant for treatment of major depressive disorder: a novel negative allosteric modulator of metabotropic glutamate receptor 5

Expert Opinion on Investigational Drugs ◽

10.1517/13543784.2015.1074175 ◽

2015 ◽

Vol 24 (9) ◽

pp. 1247-1260 ◽

Cited By ~ 25

Author(s):

Kjell Fuxe ◽

Dasiel O Borroto-Escuela

Keyword(s):

Major Depressive Disorder ◽

Depressive Disorder ◽

Glutamate Receptor ◽

Allosteric Modulator ◽

Major Depressive ◽

Metabotropic Glutamate ◽

Efficacy, tolerability and pharmacokinetics of a modified release formulation of ADX10059, a negative allosteric modulator of metabotropic glutamate receptor 5: an esophageal pH-impedance study in healthy subjects

Neurogastroenterology & Motility ◽

10.1111/j.1365-2982.2010.01484.x ◽

2010 ◽

Vol 22 (8) ◽

pp. 859-e231 ◽

Cited By ~ 32

Author(s):

F. Zerbib ◽

C. Keywood ◽

G. Strabach

Keyword(s):

Glutamate Receptor ◽

Healthy Subjects ◽

Allosteric Modulator ◽

Modified Release ◽

Release Formulation ◽

Metabotropic Glutamate ◽

Esophageal Ph ◽

Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.6b01858 ◽

2017 ◽

Vol 60 (6) ◽

pp. 2470-2484 ◽

Cited By ~ 12

Author(s):

János Galambos ◽

Attila Bielik ◽

Mikhail Krasavin ◽

Zoltán Orgován ◽

György Domány ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

Pharmacology of Basimglurant (RO4917523, RG7090), a Unique Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator in Clinical Development for Depression

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.114.222463 ◽

2015 ◽

Vol 353 (1) ◽

pp. 213-233 ◽

Cited By ~ 62

Author(s):

Lothar Lindemann ◽

Richard H. Porter ◽

Sebastian H. Scharf ◽

Basil Kuennecke ◽

Andreas Bruns ◽

...

Keyword(s):

Glutamate Receptor ◽

Clinical Development ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

Faculty Opinions recommendation of Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.718229898.793490069 ◽

2014 ◽

Author(s):

John Lowe

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

In Vitro Functional Characterization of GET73 as Possible Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5

Frontiers in Pharmacology ◽

10.3389/fphar.2018.00327 ◽

2018 ◽

Vol 9 ◽

Cited By ~ 1

Author(s):

Sarah Beggiato ◽

Andrea C. Borelli ◽

Maria C. Tomasini ◽

M. Paola Castelli ◽

Nicholas Pintori ◽

...

Keyword(s):

Glutamate Receptor ◽

Functional Characterization ◽

Allosteric Modulator ◽

Metabotropic Glutamate ◽

A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease

Gut ◽

10.1136/gut.2008.162040 ◽

2009 ◽

Vol 58 (9) ◽

pp. 1192-1199 ◽

Cited By ~ 88

Author(s):

C Keywood ◽

M Wakefield ◽

J Tack

Keyword(s):

Glutamate Receptor ◽

Reflux Disease ◽

Oesophageal Reflux ◽

Allosteric Modulator ◽

Proof Of Concept ◽

Concept Study ◽

Metabotropic Glutamate ◽