(Q30472643)

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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

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scholarly article

1 reference

Europe PubMed Central

30 September 2017

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 (English)

1 reference

Europe PubMed Central

30 September 2017

Colleen M. Niswender

17

object named as

Colleen M Niswender

1 reference

Europe PubMed Central

30 September 2017

Craig W. Lindsley

18

object named as

Craig W Lindsley

1 reference

Europe PubMed Central

30 September 2017

P. Jeffrey Conn

20

object named as

P Jeffrey Conn

1 reference

Europe PubMed Central

30 September 2017

13

object named as

Usha N Menon

1 reference

Europe PubMed Central

30 September 2017

Alice L. Rodriguez

1

object named as

Alice L Rodriguez

1 reference

Europe PubMed Central

30 September 2017

10

object named as

Emily L Days

1 reference

Europe PubMed Central

30 September 2017

Shaun R Stauffer

16

object named as

Shaun R Stauffer

1 reference

Europe PubMed Central

30 September 2017

6

object named as

Randy L Smith

1 reference

Europe PubMed Central

30 September 2017

3

object named as

Carrie K Jones

1 reference

Europe PubMed Central

30 September 2017

author name string

Mark D Grier

2

1 reference

Europe PubMed Central

30 September 2017

Elizabeth J Herman

4

1 reference

Europe PubMed Central

30 September 2017

Alexander S Kane

5

1 reference

Europe PubMed Central

30 September 2017

Richard Williams

7

1 reference

Europe PubMed Central

30 September 2017

Ya Zhou

8

1 reference

Europe PubMed Central

30 September 2017

Joy E Marlo

9

1 reference

Europe PubMed Central

30 September 2017

Tasha N Blatt

11

1 reference

Europe PubMed Central

30 September 2017

Satyawan Jadhav

12

1 reference

Europe PubMed Central

30 September 2017

Paige N Vinson

14

1 reference

Europe PubMed Central

30 September 2017

Jerri M Rook

15

1 reference

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30 September 2017

C David Weaver

19

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30 September 2017

language of work or name

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publication date

5 October 2010

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30 September 2017

Molecular Pharmacology

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30 September 2017

78

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30 September 2017

6

1 reference

Europe PubMed Central

30 September 2017

1105-1123

1 reference

Europe PubMed Central

30 September 2017

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

1 reference

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20 June 2018

Metabotropic glutamate receptors: physiology, pharmacology, and disease

1 reference

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20 June 2018

Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonist

1 reference

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A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning

1 reference

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20 June 2018

mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning

1 reference

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20 June 2018

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273

1 reference

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20 June 2018

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

1 reference

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20 June 2018

Positive allosteric modulation of mGluR5 receptors facilitates extinction of a cocaine contextual memory

1 reference

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20 June 2018

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

1 reference

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20 June 2018

Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

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 activiti

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

mGluR5 antagonists: discovery, characterization and drug development.

1 reference

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20 June 2018

Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

1 reference

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20 June 2018

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors

1 reference

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20 June 2018

N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2993468

20 June 2018

Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia

1 reference

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20 June 2018

A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators

1 reference

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20 June 2018

A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators

1 reference

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20 June 2018

Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity

1 reference

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20 June 2018

Metabotropic glutamate receptors as novel targets for anxiety and stress disorders

1 reference

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Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

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20 June 2018

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models

1 reference

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20 June 2018

Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo

1 reference

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20 June 2018

The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety

1 reference

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The mGluR theory of fragile X mental retardation

1 reference

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20 June 2018

Targeting metabotropic glutamate receptors for treatment of the cognitive symptoms of schizophrenia

1 reference

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A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain

1 reference

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Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine

1 reference

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20 June 2018

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

1 reference

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

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[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.

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

1 reference

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Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system

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20 June 2018

3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity

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Localization and physiological roles of metabotropic glutamate receptors in the direct and indirect pathways of the basal ganglia

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Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives.

1 reference

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Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site

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2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

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5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity

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The mGluR5 antagonist MPEP, but not the mGluR2/3 agonist LY314582, augments PCP effects on prepulse inhibition and locomotor activity

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26 November 2018

Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents.

1 reference

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The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate recepto

1 reference

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12 December 2020

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10.1124/MOL.110.067207

1 reference

Europe PubMed Central

30 September 2017

1 reference

Europe PubMed Central

30 September 2017

1 reference

Europe PubMed Central

30 September 2017

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