In Vivo Ketamine-Induced Changes in [11C]ABP688 Binding to Metabotropic Glutamate Receptor Subtype 5
Keywords: Brain; [11C]ABP688; Glutamate; Ketamine; mGluR5; PET;
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Age-related testicular toxicity of mGluR5 negative allosteric modulators appears to be unrelated to testis drug transporter maturity
Keywords: Testis; mGluR5; Immaturity; Drug transporter; Rat;
Blockade of metabotropic glutamate receptor 5 protects against DNA damage in a rotenone-induced Parkinson's disease model
Keywords: DHPG; (s)-3,5- dihydroxy-phenylglycine; DMSO; dimethylsulfoxide; ERK; extracellular signal-regulated kinase; MAPK; mitogen-activated protein kinase; mGluR5; metabotropic glutamate receptor 5; MPEP; 2-methyl-6-(phenylethynyl)pyridine; PD; Parkinson's dis
GABA receptor subunit distribution and FMRP-mGluR5 signaling abnormalities in the cerebellum of subjects with schizophrenia, mood disorders, and autism
Keywords: GABA; Schizophrenia; Bipolar disorder; Cerebellum; FMRP; mGluR5;
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Hit-to-lead optimization
Keywords: mGluR5; Negative allosteric modulator;
Preparation of the metabotropic glutamate receptor 5 (mGluR5) PET tracer [18F]FPEB for human use: An automated radiosynthesis and a novel one-pot synthesis of its radiolabeling precursor
Keywords: [18F]FPEB; mGluR5; Radiotracer synthesis; PET; Suzuki coupling;
New insights into the molecular pathophysiology of fragile X syndrome and therapeutic perspectives from the animal model
Keywords: Autism; Fragile X syndrome; mGluR5; Mammalian target of rapamycin (mTOR); Endocannabinoid system; CB1 cannabinoid receptor; Intellectual disability; Anxiety; Epilepsy; Nociception;
Spinal administration of mGluR5 antagonist prevents the onset of bortezomib induced neuropathic pain in rat
Keywords: Bortezomib; Neuropathy; Metabotropic glutamate receptor; glutamate reuptake; Hyperalgesia; BINP; Bortezomib induced neuropathy; MPEP; Methyl-6-(phenylethynyl)-pyridine; mGluR5; Metabotropic glutamate receptor 5; SNCV; sensory nerve conduction velocity;
Haloperidol-induced Nur77 expression in striatopallidal neurons is under the control of protein phosphatase 1 regulation by DARPP-32
Keywords: Striatum; Dopamine; Orphan nuclear receptors; Antipsychotics; A2AR; adenosine 2A receptor; CDK5; cyclin-dependent kinase 5; DAPI; 4â²,6â²-Diamidino-2-phenylindole; DARPP-32; dopamine- and cAMP-regulated phosphoprotein of 32Â kDa; D1R, D2R, and D3R; dopa
Reduced excitatory amino acid transporter 1 and metabotropic glutamate receptor 5 expression in the cerebellum of fragile X mental retardation gene 1 premutation carriers with fragile X-associated tremor/ataxia syndrome
Keywords: FMR1; FMRP; Premutation; Fragile X tremor/ataxia syndrome; FXTAS; Glu transporters; EAAT1; EAAT2; mGluR5;
Pre-ischemic treadmill training alleviates brain damage via GLT-1-mediated signal pathway after ischemic stroke in rats
Keywords: CCA, common carotid artery; DW, dry weight; EAAT, excitatory amino acids transporter; ECA, external carotid artery; ERK1/2, event-related kinase 1/2; ICA, internal carotid artery; MCA, middle cerebral artery; MCAO, middle cerebral artery occlusion; mGluR5
Disrupted in Schizophrenia 1 Modulates Medial Prefrontal Cortex Pyramidal Neuron Activity Through cAMP Regulation of Transient Receptor Potential C and Small-Conductance K+ Channels
Keywords: Ca2 waves; DISC1; IP3; mGluR5; persistent activity; prefrontal cortex
Knocking down metabotropic glutamate receptor 1 improves survival and disease progression in the SOD1G93A mouse model of amyotrophic lateral sclerosis
Keywords: ALS; amyotrophic lateral sclerosis; AMPA; α-amino-3-hydroxy-5-methyl-4-isoxazole propionate; [3H]d-Asp; [3H]d-aspartate; CAT; catalase; 3,5-DHPG; (S)-3,5-dihydroxyphenylglycine; Gapdh; Glyceraldehyde 3-phosphate dehydrogenase; Glu; glutamate; LTR; long t
The different effects of LPS and poly I:C prenatal immune challenges on the behavior, development and inflammatory responses in pregnant mice and their offspring
Keywords: Behavior; Cytokines; Development; Immune response; Inflammation; mGluR5
AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: Identification, SAR and pharmacological characterization
Keywords: [Ca2+]i; intracellular Ca2+ concentration; CDZ; chlordiazepoxide; 95% CI; 95-percent confidence interval (as obtained with best-curve fitting); FLIPR; Fluorescence Imaging Plate Reader⢠(assay); GABAB; gamma-amino butyric acid receptor, subtype B; l-Glu
mGluR5 is necessary for maintenance of methamphetamine-induced associative learning
Keywords: Conditioned place preference; Metabotropic glutamate receptor; mGluR5; mGluR1; Rat;
Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators
Keywords: mGluR5; Negative allosteric modulator;
Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1
Keywords: mGluR5; Positive allosteric modulator; PAM; CB1; Prefrontal cortex; Synaptic transmission;
Different effects of the NMDA receptor antagonists ketamine, MK-801, and memantine on postsynaptic density transcripts and their topography: Role of Homer signaling, and implications for novel antipsychotic and pro-cognitive targets in psychosis
Keywords: ACC; anterior cingulate cortex; ANOVA; one-way analysis of variance; Arc; activity-related cytoplasmic protein; BDNF; brain-derived neurotrophic factor; core; core of the nucleus accumbens; DEPC; diethylpyrocarbonate; dlCP; dorsolateral caudate putamen; d
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators
Keywords: CIZDIEPYKQXGQG-UHFFFAOYSA-N; OFNVYYXEOJUGRH-UHFFFAOYSA-N; SONLNLJEFBMKGV-UHFFFAOYSA-N; Metabotropic glutamate receptor; mGluR5; Allosteric modulator; Scaffold hopping; AFQ-056;
Novelty-Seeking Behaviors and the Escalation of Alcohol Drinking After Abstinence in Mice Are Controlled by Metabotropic Glutamate Receptor 5 on Neurons Expressing Dopamine D1 Receptors
Keywords: Alcohol abuse; dopamine receptor D1; mGluR5; novelty seeking; reward; sensation seeking
Discovery, synthesis, and structure–activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators
Keywords: Metabotropic glutamate receptor; mGluR5; Allosteric modulator; Virtual screening; l-DOPA induced dyskinesia
Neurophysiological signals as potential translatable biomarkers for modulation of metabotropic glutamate 5 receptors
Keywords: Polysomnography; Quantitative electroencephalography; mGluR5; Rat; Anxietyσemg, standard deviation of the EMG amplitude; AFQ056, methyl (3aR,4S,7aR)-4-hydroxy-4-[(3-methylphenyl)ethynyl]octahydro-1H-indole-1-carboxylate; AP, Anterior Posterior; DV, Dorsal
Aβ leads to Ca2+ signaling alterations and transcriptional changes in glial cells
Keywords: Glial cells; Amyloid beta; Alzheimer's disease; Calcium deregulation; mGluR5; IP3R1; Calcineurin
mGluR5 knockout mice display increased dendritic spine densities
Keywords: Barrel cortex; mGluR5; Dendritic spines
Hippocampal mGluR5 predicts an occurrence of helplessness behavior after repetitive exposure to uncontrollable stress
Keywords: mGluR5; Helplessness; Coping strategy; Stress; Rat;
The mGlu5 receptor antagonist MTEP attenuates opiate self-administration and cue-induced opiate-seeking behaviour in mice
Keywords: Reinstatement; Morphine; Intra-venous self-administration; Drug-seeking; MGluR5; Opiates; Relapse;
The mGlu5 receptor antagonist MPEP activates specific stress-related brain regions and lacks neurotoxic effects of the NMDA receptor antagonist MK-801: Significance for the use as anxiolytic/antidepressant drug
Keywords: mGluR5; c-Fos; Stress-related areas; Neurotoxicity; Antidepressants; Anxiolytics
Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists
Keywords: Glutamate; Excitatory amino acid; Metabotropic glutamate receptor; mGluR5; Negative allosteric modulator; 1H-pyrrolo[2,3-c]pyridine-7-carboxamides
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development
Keywords: mGluR5; Negative allosteric modulator; GPCR; In vitro pharmacology; Pain; Clinical candidate;
mGluR5 receptors in the basolateral amygdala and nucleus accumbens regulate cue-induced reinstatement of ethanol-seeking behavior
Keywords: Ethanol; Self-administration; Reinstatement glutamate; mGluR5; Antagonist; Cue;
Neuropharmacology and AnalgesiaInvestigation of the antidyskinetic site of action of metabotropic and ionotropic glutamate receptor antagonists. Intracerebral infusions in 6-hydroxydopamine-lesioned rats with levodopa-induced dyskinesia
Keywords: LID (levodopa-induced dyskinesia); Metabotropic glutamate receptor antagonist; NMDA; AMPA; mGluR5; Intracerebral infusion;
Metabotropic glutamate receptor 5 modulates behavioral and hypothermic responses to toluene in rats
Keywords: Toluene; mGluR5; NMDA receptor; Motor coordination; Learning; Hypothermia;
Pharmacological interference with metabotropic glutamate receptor subtype 7 but not subtype 5 differentially affects within- and between-session extinction of Pavlovian conditioned fear
Keywords: AMN082; DCS; Fear extinction; L-glutamate; MPEP; mGluR5; mGluR7;
Differential involvement of mGluR1 and mGluR5 in memory reconsolidation and retrieval in a passive avoidance task in 1-day old chicks
Keywords: mGluR1; mGluR5; Memory reconsolidation; Retrieval; Chicks;
Gating of NMDA receptor-mediated hippocampal spike timing-dependent potentiation by mGluR5
Keywords: Hippocampus; mGluR5; Spike timing-dependent plasticity; CA1; Development; Rat;
Transient nerve root compression load and duration differentially mediate behavioral sensitivity and associated spinal astrocyte activation and mGLuR5 expression
Keywords: astrocyte; biomechanics; mGluR5; nerve root; pain; radicularANOVA, analysis of variance; GFAP, glial fibrillary acidic protein; MAP2, microtubule-assocated protein; mGluRs, G protein-coupled metabotropic receptors
The Effect of N-Acetylcysteine in the Nucleus Accumbens on Neurotransmission and Relapse to Cocaine
Keywords: Addiction; cocaine; mGluR2/3; mGluR5; N-acetylcysteine; nucleus accumbens
The increased expression of metabotropic glutamate receptor 5 in subventricular zone neural progenitor cells and enhanced neurogenesis in a rat model of intracerebral hemorrhage
Keywords: mGluR5; CHPG; intracerebral hemorrhage; neurogenesis; rat; BDNF; brain derived neurophic factor; bFGF; basic fibroblast growth factor; BMSCs; bone marrow derived stroma cells; BrdU; 5-bromo-2â²-deoxyuridine; CHPG; (R,S)-2-chloro-5-hydroxyphenylglycine; C
Peripheral nerve injury produces a sustained shift in the balance between glutamate release and uptake in the dorsal horn of the spinal cord
Keywords: Glutamate release; mGluR5; Glutamate uptake; Spinal dorsal horn; Neuropathic pain;
Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype
Keywords: Glutamate; mGluR5; Allosteric modulator; PAM; NAM; Efficacy switching
Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5
Keywords: mGluR5; MPEP; CDPPB; Allosteric modulators
Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series
Keywords: Glutamate; mGluR5; MPEP; Antagonist
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: Hit to lead studies
Keywords: mGluR5; Negative allosteric modulator; Anxiolytic; LipE;
The mTOR signaling pathway in the prefrontal cortex is compromised in major depressive disorder
Keywords: MDD; major depressive disorder; PFC; prefrontal cortex; NMDA; N-methyl-d-aspartate; NR2A; NMDA receptor subunit 2A; NR2B; NMDA receptor subunit 2B; mGluR5; metabotropic glutamate receptor subtype 5; PSD-95; postsynaptic density-95Â kDa; mTOR; mammalian ta
Positive allosteric modulation of metabotropic glutamate receptor 5 down-regulates fibrinogen-activated microglia providing neuronal protection
Keywords: BBB; blood brain barrier; CDPPB; 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide; CGC; cerebellar granule cells; CNS; central nervous system; DCGIV; (2S,2â²R,3â²R)-2-(2â²,3â²-dicarboxycyclopropyl)glycine; ERK1/2; extracellular signal-regulated kinas
The acute antiparkinsonian and antidyskinetic effect of AFQ056, a novel metabotropic glutamate receptor type 5 antagonist, in l-Dopa-treated parkinsonian monkeys
Keywords: mGluR5; Dyskinesia; Levodopa; Parkinson; MPTP monkey; AFQ056
In vitro and in vivo evaluation of [18F]-FDEGPECO as a PET tracer for imaging the metabotropic glutamate receptor subtype 5 (mGluR5)
Keywords: Autoradiography; Biodistribution; PET imaging; mGluR5; [18F]-FDEGPECO;
The neurochemical basis for the treatment of autism spectrum disorders and Fragile X Syndrome
Keywords: Cerebellum; GABA; GABA(A); GABA(B); GTPase; Metabotropic glutamate; mGluR5; Neurodevelopmental; Dendritic spines
Metabotropic glutamate receptor type 5 in levodopa-induced motor complications
Keywords: Glutamate receptor; mGluR5; Human; MPTP monkey; Wearing-off; Dyskinesias