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1. Full Text 321. Watching Synapses in Action: From Assaying Synaptic Function to Drug Discovery
by Kashikar, Nachiket and Kemp, John and Lavreysen, Hilde
Biological Psychiatry, ISSN 0006-3223, 05/2017, Volume 81, Issue 10, pp. S132 - S132
Drug discovery
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2. Full Text Watching Synapses in Action: From Assaying Synaptic Function to Drug Discovery
by Kashikar, Nachiket and Kemp, John and Lavreysen, Hilde
Biological Psychiatry, ISSN 0006-3223, 2017, Volume 81, Issue 10, pp. S132 - S132
Psychiatry | Drug discovery
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3. Therapeutic potential of group III metabotropic glutamate receptors
by Lavreysen, Hilde and Dautzenberg, Frank M
Current Medicinal Chemistry, ISSN 0929-8673, 03/2008, Volume 15, Issue 7, pp. 671 - 684
Metabotropic glutamate (mGlu) receptors have received much attention, driven by a strong belief in the potential of these modulatory glutamate receptors as... 
Glutamate | Receptor | Metabotropic | CHEMISTRY, MEDICINAL | PHARMACOLOGICAL CHARACTERIZATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | PROTEIN-COUPLED RECEPTORS | MGLU8 RECEPTOR | metabotropic | MICE LACKING | receptor | MESSENGER-RNA | ANXIETY-RELATED BEHAVIOR | EPILEPSY-PRONE RATS | ANXIOLYTIC-LIKE | POSITIVE ALLOSTERIC MODULATORS | PHARMACOLOGY & PHARMACY | glutamate | PRIMARY AFFERENT TERMINALS | Ligands | Structure-Activity Relationship | Animals | Receptors, Metabotropic Glutamate - agonists | Humans | Receptors, Metabotropic Glutamate - antagonists & inhibitors
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4. Full Text 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
by Metcalf, Cameron S and Klein, Brian D and Smith, Misty D and Ceusters, Marc and Lavreysen, Hilde and Pype, Stefan and Van Osselaer, Nancy and Twyman, Roy and White, H. Steve
Epilepsia, ISSN 0013-9580, 03/2018, Volume 59, Issue 3, pp. 724 - 735
Summary Objective We previously demonstrated that positive allosteric modulators (PAMs) of metabotropic glutamate subtype 2 (mGlu2) receptors have potential... 
metabotropic glutamate receptors | animal models | isobologram | combination studies | psychomotor seizures | EFFICACY | PHARMACOLOGICAL CHARACTERIZATION | SEIZURE MODEL | 6 HZ MODEL | COMBINATION | GABAPENTIN | MGLU2 RECEPTORS | DISCOVERY | CLINICAL NEUROLOGY | MICE | ANTIEPILEPTIC DRUGS | Medical research | Anticonvulsants | Analysis | Epilepsy | Medicine, Experimental | Amino acids | Seizures (Medicine) | Glutamate | Cornea | Kindling | Glutamic acid receptors | Valproic acid | Etiracetam | Allosteric properties | Sodium | Plasma levels | Sodium valproate | Glutamic acid receptors (metabotropic) | Lamotrigine | Seizures | Index Medicus
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5. Full Text MGlu2 receptor agonism, but not positive allosteric modulation, elicits rapid tolerance towards their primary efficacy on sleep measures in rats
by Ahnaou, Abdallah and Lavreysen, Hilde and Tresadern, Gary and Cid, Jose M and Drinkenburg, Wilhelmus H
PLoS ONE, ISSN 1932-6203, 12/2015, Volume 10, Issue 12, p. e0144017
G-protein-coupled receptor (GPCR) agonists are known to induce both cellular adaptations resulting in tolerance to therapeutic effects and withdrawal symptoms... 
METABOTROPIC GLUTAMATE-RECEPTOR | SUPRACHIASMATIC NUCLEUS | MOOD DISORDERS | PHARMACOLOGICAL CHARACTERIZATION | MULTIDISCIPLINARY SCIENCES | ACETYLCHOLINE-RELEASE | CENTRAL-NERVOUS-SYSTEM | GROUP-II | PREFRONTAL CORTEX | REM-SLEEP | AMYGDALA | Cricetulus | Sleep, REM - physiology | Allosteric Regulation | Humans | Male | Receptors, Metabotropic Glutamate - metabolism | Bridged Bicyclo Compounds - adverse effects | Receptors, Metabotropic Glutamate - genetics | Cell Membrane - metabolism | Cell Membrane - drug effects | CHO Cells | Binding, Competitive | Recombinant Proteins - metabolism | Sleep, REM - drug effects | Gene Expression | Triazines - pharmacology | Drug Administration Schedule | Allosteric Site - drug effects | Drug Tolerance | Rats | Recombinant Proteins - genetics | Rats, Sprague-Dawley | Animals | Protein Binding | Wakefulness - physiology | Excitatory Amino Acid Agonists - adverse effects | Ligands | Molecular Docking Simulation | Pyridines - pharmacology | Structural Homology, Protein | Receptors, Metabotropic Glutamate - agonists | Physiological aspects | Cell receptors | Genetic aspects | Sleep | Research | Adaptations | Drugs | Neurosciences | Substance abuse treatment | G protein-coupled receptors | Mental disorders | Sleep (REM) | Glutamic acid receptors | Selectivity | Rapid eye movement state | Eye movements | Recovery | Proteins | Receptors | Allosteric properties | Antidepressants | Rodents | Modulation | Docking | Drug dosages | Sleep and wakefulness | Pharmaceutical sciences | Translation | Effectiveness | Withdrawal | Research & development--R&D | Latency | Studies | Brain research | In vivo methods and tests | Psychiatry | Glutamic acid receptors (metabotropic) | Neurotransmission | Binding sites | Chronic effects | Research & development | R&D
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6. Full Text Efficacy of mGlu2‐positive allosteric modulators alone and in combination with levetiracetam in the mouse 6 Hz model of psychomotor seizures
by Metcalf, Cameron S and Klein, Brian D and Smith, Misty D and Pruess, Tim and Ceusters, Marc and Lavreysen, Hilde and Pype, Stefan and Van Osselaer, Nancy and Twyman, Roy and White, H. Steve
Epilepsia, ISSN 0013-9580, 03/2017, Volume 58, Issue 3, pp. 484 - 493
Summary Objective The metabotropic glutamate receptor subtype 2 (mGlu2) possesses both orthosteric and allosteric modulatory sites, are expressed in the... 
Metabotropic glutamate receptors | Animal models | Psychomotor seizures | Combination studies | Levetiracetam | Anticonvulsants | Seizures (Medicine) | Glutamate | Analysis | Epilepsy | Convulsions & seizures | Index Medicus
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7. Full Text Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ‐46281222
by Doornbos, Maarten L J and Pérez‐Benito, Laura and Tresadern, Gary and Mulder‐Krieger, Thea and Biesmans, Ilse and Trabanco, Andrés A and Cid, Jose María and Lavreysen, Hilde and IJzerman, Adriaan P and Heitman, Laura H
British Journal of Pharmacology, ISSN 0007-1188, 02/2016, Volume 173, Issue 3, pp. 588 - 600
Background and Purpose Allosteric modulation of the mGlu2 receptor is a potential strategy for treatment of various neurological and psychiatric disorders.... 
STRUCTURAL INSIGHTS | POTENT | ACTIVATION | MGLUR2 | DETERMINANTS | PHARMACOLOGICAL CHARACTERIZATION | PHARMACOLOGY & PHARMACY | HEPTAHELICAL DOMAIN | SIMULATIONS | BINDING | DISCOVERY | Allosteric Regulation - drug effects | Triazoles - pharmacology | Animals | Cricetulus | Piperidines - pharmacology | Receptors, Metabotropic Glutamate - genetics | Humans | Models, Molecular | Pyridines - pharmacology | Receptors, Metabotropic Glutamate - metabolism | CHO Cells | Analysis | Amino acids | Drug discovery | G proteins | Glutamate | Mental illness | Protein binding | Mutagenesis | Binding sites | GTP | Mental disorders | Computer simulation | Computational neuroscience | Molecular dynamics | Homology | Glutamic acid receptors | Activation | Neurological diseases | Proteins | Allosteric properties | Receptors | Dynamic tests | Site-directed mutagenesis | Modulation | Computer applications | Glutamic acid receptors (metabotropic) | Index Medicus | Research Papers | Research Paper
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8. Full Text Molecular Switches of Allosteric Modulation of the Metabotropic Glutamate 2 Receptor
by Pérez-Benito, Laura and Doornbos, Maarten L.J and Cordomí, Arnau and Peeters, Luc and Lavreysen, Hilde and Pardo, Leonardo and Tresadern, Gary
Structure, ISSN 0969-2126, 07/2017, Volume 25, Issue 7, pp. 1153 - 1162.e4
Metabotropic glutamate (mGlu) receptors are class C G protein-coupled receptors (GPCRs) crucial for CNS function and important drug discovery targets.... 
mGlu | GPCR | class C | NAM | transmission switch | molecular dynamics | activation | PAM | mGluR | allosteric modulator | ACTIVATION | PHARMACOLOGICAL CHARACTERIZATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | PROTEIN-COUPLED RECEPTORS | TRANSMEMBRANE DOMAIN | IDENTIFICATION | DISCOVERY | CELL BIOLOGY | POTENT | BIOPHYSICS | BINDING | MGLU2 RECEPTOR | AGONIST | Cricetinae | Cricetulus | Allosteric Regulation | Humans | Receptors, Metabotropic Glutamate - metabolism | Triazoles - pharmacology | Animals | Biphenyl Compounds - pharmacology | Piperidines - pharmacology | Receptors, Metabotropic Glutamate - genetics | Allosteric Site | Protein Binding | Ligands | Pyridines - pharmacology | Mutation | Receptors, Metabotropic Glutamate - chemistry | CHO Cells | Indans - pharmacology | Amino acids | Drug discovery | G proteins | Glutamate | Molecular dynamics | Resveratrol
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9. Full Text Biased mGlu 5 -Positive Allosteric Modulators Provide InVivo Efficacy without Potentiating mGlu 5 Modulation of NMDAR Currents
by Rook, Jerri M and Xiang, Zixiu and Lv, Xiaohui and Ghoshal, Ayan and Dickerson, Jonathan W and Bridges, Thomas M and Johnson, Kari A and Foster, Daniel J and Gregory, Karen J and Vinson, Paige N and Thompson, Analisa D and Byun, Nellie and Collier, Rebekah L and Bubser, Michael and Nedelcovych, Michael T and Gould, Robert W and Stauffer, Shaun R and Daniels, J. Scott and Niswender, Colleen M and Lavreysen, Hilde and Mackie, Claire and Conde-Ceide, Susana and Alcazar, Jesus and Bartolomé-Nebreda, José M and Macdonald, Gregor J and Talpos, John C and Steckler, Thomas and Jones, Carrie K and Lindsley, Craig W and Conn, P. Jeffrey
Neuron, ISSN 0896-6273, 05/2015, Volume 86, Issue 4, pp. 1029 - 1040
Schizophrenia is associated with disruptions in N-methyl-D-aspartate glutamate receptor subtype (NMDAR)-mediated excitatory synaptic signaling. The... 
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10. Full Text Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2
by Doornbos, Maarten L.J and Vermond, Sophie C and Lavreysen, Hilde and Tresadern, Gary and IJzerman, Adriaan P and Heitman, Laura H
Biochemical Pharmacology, ISSN 0006-2952, 09/2018, Volume 155, pp. 356 - 365
While many orthosteric ligands have been developed for the mGlu receptor, little is known about their target binding kinetics and how these relate to those of... 
Binding kinetics | Glutamate | Allosteric modulation | Orthosteric | mGlu2 receptor | mGlu | receptor | MOLECULAR-MECHANISM | EFFICACY | PHARMACOLOGICAL CHARACTERIZATION | DRUG DISCOVERY | PROTEIN-COUPLED RECEPTORS | MUSCARINIC M-3 RECEPTOR | MAJOR DEPRESSION | TARGET BINDING | mGlu receptor | PHARMACOLOGY & PHARMACY | RAT-BRAIN | MGLU2 RECEPTOR | Amino acids | Drug discovery
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11. Full Text Preclinical evaluation of the antipsychotic potential of the mGlu2‐positive allosteric modulator JNJ‐40411813
by Lavreysen, Hilde and Langlois, Xavier and Donck, Luc Ver and Nuñez, José María Cid and Pype, Stefan and Lütjens, Robert and Megens, Anton
Pharmacology Research & Perspectives, ISSN 2052-1707, 03/2015, Volume 3, Issue 2, pp. 1 - n/a
JNJ‐40411813/ADX71149 (1‐butyl‐3‐chloro‐4‐(4‐phenylpiperidin‐1‐yl) pyridin‐2(1H)‐one) is a positive allosteric modulator (PAM) of the mGlu2 receptor, which... 
antipsychotic‐like activity | 5HT2A receptor antagonist | LY404039 | ritanserin | JNJ‐40411813 | JNJ‐42153605 | PAM | mGlu2 | 5HT | JNJ-40411813 | MGlu2 | receptor antagonist | Antipsychotic-like activity | JNJ-42153605 | Ritanserin | Studies | Psychotropic drugs | Hypotheses | Animals | Authorship | Research & development--R&D | Schizophrenia | Ligands | Variance analysis | Drug dosages | Binding sites | antipsychotic-like activity | Original
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12. Full Text Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization
by Doornbos, Maarten L. J and Wang, Xuesong and Vermond, Sophie C and Peeters, Luc and Pérez-Benito, Laura and Trabanco, Andrés A and Lavreysen, Hilde and Cid, José María and Heitman, Laura H and Tresadern, Gary and Ijzerman, Adriaan P
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2019, Volume 62, Issue 1, pp. 223 - 233
Covalent labeling of G protein-coupled receptors (GPCRs) by small molecules is a powerful approach to understand binding modes, mechanism of action,... 
MOLECULAR-MECHANISM | JNJ-40411813 | POTENT | CHEMISTRY, MEDICINAL | LIGANDS | KINETICS | MODULATOR | POINT | MGLU2 RECEPTOR | DISCOVERY | AGONIST | Index Medicus
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13. Full Text [3H]R214127: A Novel High-Affinity Radioligand for the mGlu1 Receptor Reveals a Common Binding Site Shared by Multiple Allosteric Antagonists
by Hilde Lavreysen and Cor Janssen and François Bischoff and Xavier Langlois and Josée E. Leysen and Anne S. J. Lesage
Molecular Pharmacology, ISSN 0026-895X, 05/2003, Volume 63, Issue 5, pp. 1082 - 1093
R214127 was shown to be a potent and noncompetitive metabotropic glutamate 1 (mGlu1) receptor-selective antagonist. The kinetics and pharmacology of [ 3... 
HIPPOCAMPUS | METABOTROPIC GLUTAMATE-RECEPTOR | POTENT | CPCCOET | SUBTYPES | IMMUNOHISTOCHEMICAL LOCALIZATION | LONG-TERM DEPRESSION | PHARMACOLOGY & PHARMACY | RAT-BRAIN | CELLULAR-LOCALIZATION | SPLICE VARIANTS | Allosteric Regulation | Humans | Tritium | Quinolines - pharmacology | Brain - metabolism | Quinoxalines - pharmacology | Transfection | Cell Membrane - metabolism | Radioligand Assay | Chromones - pharmacology | Binding Sites | Pyrans - pharmacology | Cell Membrane - drug effects | Adamantane - analogs & derivatives | CHO Cells | Binding, Competitive | Cell Line | Adamantane - pharmacology | Cricetinae | Rats | Naphthalenes - pharmacology | Brain - drug effects | Animals | Receptors, Metabotropic Glutamate - antagonists & inhibitors | Quisqualic Acid - pharmacology
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14. Full Text mGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats
by Megens, Anton A.H.P and Hendrickx, Herman M.R and Hens, Koen A and Talloen, Willem J.-P.E and Lavreysen, Hilde
European Journal of Pharmacology, ISSN 0014-2999, 03/2014, Volume 727, Issue 1, pp. 130 - 139
Inhibition of conditioned avoidance behavior in rats is generally considered predictive for antipsychotic activity in man. The present study investigated the... 
Schizophrenia | Antipsychotics | Locomotion | Allosteric modulator | mGlu2/3 | Conditioned avoidance | mGlu
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15. Full Text Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor
by Doornbos, Maarten L.J and Van der Linden, Ilse and Vereyken, Liesbeth and Tresadern, Gary and IJzerman, Adriaan P and Lavreysen, Hilde and Heitman, Laura H
Biochemical Pharmacology, ISSN 0006-2952, 06/2018, Volume 152, pp. 201 - 210
Label-free cellular assays using a biosensor provide new opportunities for studying G protein-coupled receptor (GPCR) signaling. As opposed to conventional... 
Impedance | Label-free |