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Biological Psychiatry, ISSN 0006-3223, 05/2017, Volume 81, Issue 10, pp. S132 - S132
Journal Article
Biological Psychiatry, ISSN 0006-3223, 2017, Volume 81, Issue 10, pp. S132 - S132
Journal Article
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
Journal Article
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
Journal Article
Journal Article
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... 
Journal Article
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
Journal Article
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
Journal Article
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
Journal Article
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
Journal Article
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 |