Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

Allosteric Modulator ◽

Metabotropic Glutamate ◽

Structure–activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2006.06.078 ◽

2006 ◽

Vol 16 (18) ◽

pp. 4788-4791 ◽

Cited By ~ 16

Author(s):

Peter Bach ◽

Karolina Nilsson ◽

Tor Svensson ◽

Udo Bauer ◽

Lance G. Hammerland ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate ◽

Synthesis, structure–activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2016.07.019 ◽

2016 ◽

Vol 26 (16) ◽

pp. 3866-3869 ◽

Cited By ~ 3

Author(s):

Wataru Hirose ◽

Yoshihiro Kato ◽

Takayoshi Yamamoto ◽

Momoe Kassai ◽

Makoto Takata ◽

...

Keyword(s):

Glutamate Receptor ◽

Biological Evaluation ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Design, Synthesis, and Structure−Activity Relationships of Novel Bicyclic Azole-amines as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5

Journal of Medicinal Chemistry ◽

10.1021/jm100736h ◽

2010 ◽

Vol 53 (19) ◽

pp. 7107-7118 ◽

Cited By ~ 19

Author(s):

Douglas F. Burdi ◽

Rachel Hunt ◽

Lei Fan ◽

Tao Hu ◽

Jun Wang ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulators ◽

Design Synthesis ◽

Metabotropic Glutamate ◽

Discovery, synthesis, and structure–activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2013.06.049 ◽

2013 ◽

Vol 23 (16) ◽

pp. 4493-4500 ◽

Cited By ~ 8

Author(s):

Holger Kubas ◽

Udo Meyer ◽

Bjoern Krueger ◽

Mirko Hechenberger ◽

Maksims Vanejevs ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Exploration of Allosteric Agonism Structure–Activity Relationships within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254)

Journal of Medicinal Chemistry ◽

10.1021/jm401028t ◽

2013 ◽

Vol 56 (20) ◽

pp. 7976-7996 ◽

Cited By ~ 24

Author(s):

Mark Turlington ◽

Meredith J. Noetzel ◽

Aspen Chun ◽

Ya Zhou ◽

Rocco D. Gogliotti ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Acetylene Series ◽

Structure Activity ◽

Positive Allosteric Modulators

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

Structure–activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2010.03.053 ◽

2010 ◽

Vol 18 (9) ◽

pp. 3026-3035 ◽

Cited By ~ 14

Author(s):

Peng Zhang ◽

Mu-Fa Zou ◽

Alice L. Rodriguez ◽

P. Jeffrey Conn ◽

Amy Hauck Newman

Keyword(s):

Glutamate Receptor ◽

Receptor Subtype ◽

Metabotropic Glutamate ◽

Synthesis and Structure−Activity Relationships of 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine Analogues as Potent, Noncompetitive Metabotropic Glutamate Receptor Subtype 5 Antagonists; Search for Cocaine Medications

Journal of Medicinal Chemistry ◽

10.1021/jm050570f ◽

2006 ◽

Vol 49 (3) ◽

pp. 1080-1100 ◽

Cited By ~ 61

Author(s):

Yasuyoshi Iso ◽

Ewa Grajkowska ◽

Jarda T. Wroblewski ◽

Jared Davis ◽

Nicholas E. Goeders ◽

...

Keyword(s):

Glutamate Receptor ◽

Receptor Subtype ◽

Metabotropic Glutamate ◽

ADX47273 [S-(4-Fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: A Novel Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulator with Preclinical Antipsychotic-Like and Procognitive Activities

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.108.136580 ◽

2008 ◽

Vol 327 (3) ◽

pp. 827-839 ◽

Cited By ~ 138

Author(s):

Feng Liu ◽

Steve Grauer ◽

Cody Kelley ◽

Rachel Navarra ◽

Radka Graf ◽

...

Keyword(s):

Glutamate Receptor ◽

Allosteric Modulator ◽

Positive Allosteric Modulator ◽

Metabotropic Glutamate