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

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

doi:10.1124/mol.110.067207

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

Molecular Pharmacology ◽

10.1124/mol.110.067207 ◽

2010 ◽

Vol 78 (6) ◽

pp. 1105-1123 ◽

Cited By ~ 139

Author(s):

Alice L. Rodriguez ◽

Mark D. Grier ◽

Carrie K. Jones ◽

Elizabeth J. Herman ◽

Alexander S. Kane ◽

...

Keyword(s):

Functional Diversity ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Behavioral Models ◽

Metabotropic Glutamate ◽

Antipsychotic Activity

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Relationship between In Vivo Receptor Occupancy and Efficacy of Metabotropic Glutamate Receptor Subtype 5 Allosteric Modulators with Different In Vitro Binding Profiles

Neuropsychopharmacology ◽

10.1038/npp.2014.245 ◽

2014 ◽

Vol 40 (3) ◽

pp. 755-765 ◽

Cited By ~ 22

Author(s):

Jerri M Rook ◽

Mohammed N Tantawy ◽

Mohammad S Ansari ◽

Andrew S Felts ◽

Shaun R Stauffer ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Occupancy ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

In Vitro Binding ◽

Vitro Binding

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A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral Models

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.104.079244 ◽

2004 ◽

Vol 313 (1) ◽

pp. 199-206 ◽

Cited By ~ 218

Author(s):

Gene G. Kinney ◽

Julie A. O'Brien ◽

Wei Lemaire ◽

Maryann Burno ◽

Denise J. Bickel ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Allosteric Modulator ◽

Behavioral Models ◽

Positive Allosteric Modulator ◽

Metabotropic Glutamate

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Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series ofN-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That Potentiate Receptor Function in Vivo

Journal of Medicinal Chemistry ◽

10.1021/jm049400d ◽

2004 ◽

Vol 47 (24) ◽

pp. 5825-5828 ◽

Cited By ~ 127

Author(s):

Craig W. Lindsley ◽

David D. Wisnoski ◽

William H. Leister ◽

Julie A. O'Brien ◽

Wei Lemaire ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Receptor Function ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity

Biological Psychiatry ◽

10.1016/j.biopsych.2012.09.012 ◽

2013 ◽

Vol 73 (6) ◽

pp. 501-509 ◽

Cited By ~ 71

Author(s):

Jerri M. Rook ◽

Meredith J. Noetzel ◽

Wendy A. Pouliot ◽

Thomas M. Bridges ◽

Paige N. Vinson ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Correlation of Receptor Occupancy of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Mouse Brain With In Vivo Activity of Allosteric mGluR1 Antagonists

Journal of Pharmacological Sciences ◽

10.1254/jphs.09011fp ◽

2009 ◽

Vol 110 (3) ◽

pp. 315-325 ◽

Cited By ~ 12

Author(s):

Gentaroh Suzuki ◽

Hiroko Kawagoe-Takaki ◽

Takao Inoue ◽

Toshifumi Kimura ◽

Hirohiko Hikichi ◽

...

Keyword(s):

Glutamate Receptor ◽

Mouse Brain ◽

Metabotropic Glutamate Receptor ◽

Receptor Occupancy ◽

Receptor Subtype ◽

Metabotropic Glutamate

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

European Journal of Nuclear Medicine and Molecular Imaging ◽

10.1007/s00259-010-1723-7 ◽

2011 ◽

Vol 38 (6) ◽

pp. 1083-1094 ◽

Cited By ~ 39

Author(s):

Christine DeLorenzo ◽

Matthew S. Milak ◽

Kathleen G. Brennan ◽

J. S. Dileep Kumar ◽

J. John Mann ◽

...

Keyword(s):

Positron Emission Tomography ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Positron Emission Tomography Imaging ◽

Emission Tomography ◽

Receptor Subtype ◽

Tomography Imaging ◽

Metabotropic Glutamate ◽

Positron Emission

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Hepatic ischemic injury decreases using negative allosteric modulators of metabotropic glutamate receptor subtype 5

Digestive and Liver Disease ◽

10.1016/j.dld.2018.01.085 ◽

2018 ◽

Vol 50 (1) ◽

pp. 24

Author(s):

C. Berardo ◽

V. Siciliano ◽

L.G. Di Pasqua ◽

P. Richelmi ◽

F. Nicoletti ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Ischemic Injury ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Metabotropic Glutamate

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Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2018.04.053 ◽

2018 ◽

Vol 28 (10) ◽

pp. 1679-1685 ◽

Cited By ~ 1

Author(s):

Andrew S. Felts ◽

Alice L. Rodriguez ◽

Ryan D. Morrison ◽

Anna L. Blobaum ◽

Frank W. Byers ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Metabotropic Glutamate

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Negative allosteric modulators of metabotropic glutamate receptor subtype 5 protect against hepatic ischemia/reperfusion injury

Journal of Hepatology ◽

10.1016/s0168-8278(18)30466-5 ◽

2018 ◽

Vol 68 ◽

pp. S128

Author(s):

C. Berardo ◽

V. Siciliano ◽

L.G. Di Pasqua ◽

P. Richelmi ◽

F. Nicoletti ◽

...

Keyword(s):

Reperfusion Injury ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Ischemia Reperfusion Injury ◽

Ischemia Reperfusion ◽

Receptor Subtype ◽

Allosteric Modulators ◽

Hepatic Ischemia ◽

Metabotropic Glutamate ◽

Hepatic Ischemia Reperfusion

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Synthesis, radiolabeling, in vitro and in vivo evaluation of [18F]-FPECMO as a positron emission tomography radioligand for imaging the metabotropic glutamate receptor subtype 5

Nuclear Medicine and Biology ◽

10.1016/j.nucmedbio.2009.03.005 ◽

2009 ◽

Vol 36 (6) ◽

pp. 613-622 ◽

Cited By ~ 14

Author(s):

Christophe Lucatelli ◽

Michael Honer ◽

Jean-Frédéric Salazar ◽

Tobias L. Ross ◽

P. August Schubiger ◽

...

Keyword(s):

Positron Emission Tomography ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Emission Tomography ◽

Receptor Subtype ◽

In Vivo Evaluation ◽

Metabotropic Glutamate ◽

Positron Emission

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