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Molecular Switches of Allosteric Modulation of the Metabotropic Glutamate 2 Receptor

Structure (London), 2017-07, Vol.25 (7), p.1153-1162.e4

2017

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Therapeutic potential of group III metabotropic glutamate receptors

Current medicinal chemistry, 2008-03, Vol.15 (7), p.671

2008

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mGlu2 Receptor Agonism, but Not Positive Allosteric Modulation, Elicits Rapid Tolerance towards Their Primary Efficacy on Sleep Measures in Rats

PloS one, 2015-12, Vol.10 (12), p.e0144017-e0144017

2015

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Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782

The Journal of pharmacology and experimental therapeutics, 2013-09, Vol.346 (3), p.514

2013

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Discovery of 3‑Cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3‑a]pyridine (JNJ-42153605): A Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

Journal of medicinal chemistry, 2012-10, Vol.55 (20), p.8770-8789

2012

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High-throughput Analysis of Synaptic Activity in Electrically Stimulated Neuronal Cultures

Neuroinformatics (Totowa, N.J.), 2021-10, Vol.19 (4), p.737-750

2021

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Synthesis, Evaluation, and Radiolabeling of New Potent Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 as Potential Tracers for Positron Emission Tomography Imaging

Journal of medicinal chemistry, 2012-10, Vol.55 (20), p.8685-8699

2012

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Discovery of 1‑Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)‑pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

Journal of medicinal chemistry, 2014-08, Vol.57 (15), p.6495-6512

2014

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JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist

Neuropharmacology, 2004-12, Vol.47 (7), p.961-972

2004

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Scaffold Hopping to Imidazo[1,2‑a]pyrazin-8-one Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptor

ACS omega, 2021-09, Vol.6 (35), p.22997-23006

2021

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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

Molecular pharmacology, 2003-05, Vol.63 (5), p.1082-1093

2003

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Metabotropic glutamate 1 receptor distribution and occupancy in the rat brain: a quantitative autoradiographic study using [ 3H]R214127

Neuropharmacology, 2004-04, Vol.46 (5), p.609-619

2004

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321. Watching Synapses in Action: From Assaying Synaptic Function to Drug Discovery

Biological psychiatry (1969), 2017-05, Vol.81 (10), p.S132-S132

2017

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Watching Synapses in Action: From Assaying Synaptic Function to Drug Discovery

Biological psychiatry (1969), 2017, Vol.81 (10), p.S132-S132

2017

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Potent and selective pharmacodynamic synergy between the metabotropic glutamate receptor subtype 2–positive allosteric modulator JNJ‐46356479 and levetiracetam in the mouse 6‐Hz (44‐mA) model

Epilepsia (Copenhagen), 2018-03, Vol.59 (3), p.724-735

2018

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Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor

Biochemical pharmacology, 2018-06, Vol.152, p.201-210

2018

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Discovery and Kinetic Profiling of 7‑Aryl-1,2,4-triazolo[4,3‑a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2

Journal of medicinal chemistry, 2017-08, Vol.60 (15), p.6704-6720

2017

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Efficacy of mGlu2‐positive allosteric modulators alone and in combination with levetiracetam in the mouse 6 Hz model of psychomotor seizures

Epilepsia (Copenhagen), 2017-03, Vol.58 (3), p.484-493

2017

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Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization

Journal of medicinal chemistry, 2019-01, Vol.62 (1), p.223-233

2019

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Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ‐46281222

British journal of pharmacology, 2016-02, Vol.173 (3), p.588-600

2016

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Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2

Biochemical pharmacology, 2018-09, Vol.155, p.356-365

2018

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Correction to: High‑throughput Analysis of Synaptic Activity in Electrically Stimulated Neuronal Cultures

Neuroinformatics (Totowa, N.J.), 2022-07, Vol.20 (3), p.825-825

2022

Volltextzugriff (PDF)

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function

Molecular pharmacology, 2012-02, Vol.81 (2), p.120-133

2012

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In the grey zone between epilepsy and schizophrenia: alterations in group II metabotropic glutamate receptors

Acta neurologica Belgica, 2015-09, Vol.115 (3), p.221-232

2015

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Molecular Switches of Allosteric Modulation of the Metabotropic Glutamate 2 Receptor

Therapeutic potential of group III metabotropic glutamate receptors

mGlu2 Receptor Agonism, but Not Positive Allosteric Modulation, Elicits Rapid Tolerance towards Their Primary Efficacy on Sleep Measures in Rats

Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782

Discovery of 3‑Cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3‑a]pyridine (JNJ-42153605): A Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

Discovery of 8‑Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3‑a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM)

High-throughput Analysis of Synaptic Activity in Electrically Stimulated Neuronal Cultures

Synthesis, Evaluation, and Radiolabeling of New Potent Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 as Potential Tracers for Positron Emission Tomography Imaging

Discovery of 1‑Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)‑pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist

Scaffold Hopping to Imidazo[1,2‑a]pyrazin-8-one Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptor

[3H]R214127: A Novel High-Affinity Radioligand for the mGlu1 Receptor Reveals a Common Binding Site Shared by Multiple Allosteric Antagonists

Metabotropic glutamate 1 receptor distribution and occupancy in the rat brain: a quantitative autoradiographic study using [ 3H]R214127

321. Watching Synapses in Action: From Assaying Synaptic Function to Drug Discovery

Watching Synapses in Action: From Assaying Synaptic Function to Drug Discovery

Potent and selective pharmacodynamic synergy between the metabotropic glutamate receptor subtype 2–positive allosteric modulator JNJ‐46356479 and levetiracetam in the mouse 6‐Hz (44‐mA) model

Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor

Discovery and Kinetic Profiling of 7‑Aryl-1,2,4-triazolo[4,3‑a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2

Efficacy of mGlu2‐positive allosteric modulators alone and in combination with levetiracetam in the mouse 6 Hz model of psychomotor seizures

Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization

Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ‐46281222

Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2

Correction to: High‑throughput Analysis of Synaptic Activity in Electrically Stimulated Neuronal Cultures

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function

In the grey zone between epilepsy and schizophrenia: alterations in group II metabotropic glutamate receptors

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