Gene Symbol: GRM5
Description: glutamate metabotropic receptor 5
Alias: GPRC1E, MGLUR5, PPP1R86, mGlu5, metabotropic glutamate receptor 5, glutamate receptor, metabotropic 5, protein phosphatase 1, regulatory subunit 86
Species: human
Products:     GRM5

Top Publications

  1. Oertel W, Schulz J. Current and experimental treatments of Parkinson disease: A guide for neuroscientists. J Neurochem. 2016;139 Suppl 1:325-337 pubmed publisher
    ..antagonists (istradefylline, preladenant, and tozadenant) and modulators of the metabolic glutamate receptor 5 (mGluR5 - mavoglurant) and serotonin (eltoprazine) receptors...
  2. Jarius S, Metz I, König F, Ruprecht K, Reindl M, Paul F, et al. Screening for MOG-IgG and 27 other anti-glial and anti-neuronal autoantibodies in 'pattern II multiple sclerosis' and brain biopsy findings in a MOG-IgG-positive case. Mult Scler. 2016;22:1541-1549 pubmed
    ..PKCgamma), anti-glutamate receptor delta 2 (GluRdelta2), anti-metabotropic glutamate receptor 1 (mGluR1) and anti-mGluR5, as well as for anti-glial nuclei antibodies (AGNA) and Purkinje cell antibody 2 (PCA2)...
  3. Millan M, Rivet J, Gobert A. The frontal cortex as a network hub controlling mood and cognition: Probing its neurochemical substrates for improved therapy of psychiatric and neurological disorders. J Psychopharmacol. 2016;30:1099-1128 pubmed
    ..augment transmission at N-methyl-d-aspartate receptors, and of "glutamatergic antidepressants" like ketamine, mGluR5 antagonists and positive modulators of AMPA receptors (including S47445)...
  4. Fatemi S, Folsom T. GABA receptor subunit distribution and FMRP-mGluR5 signaling abnormalities in the cerebellum of subjects with schizophrenia, mood disorders, and autism. Schizophr Res. 2015;167:42-56 pubmed publisher
    ..FMRP acts as a translational repressor and, under normal conditions, inhibits metabotropic glutamate receptor 5 (mGluR5)-mediated signaling...
  5. Martin S, Bellora N, González Vallinas J, Irimia M, Chebli K, de Toledo M, et al. Preferential binding of a stable G3BP ribonucleoprotein complex to intron-retaining transcripts in mouse brain and modulation of their expression in the cerebellum. J Neurochem. 2016;139:349-368 pubmed publisher
    ..Notably, G3BP1 seems to repress the expression of the mature Grm5 (metabotropic glutamate receptor 5) transcript, by promoting the retention of an intron in the immature transcript in the cerebellum...
  6. Frederikse P, Nandanoor A, Kasinathan C. Fragile X Syndrome FMRP Co-localizes with Regulatory Targets PSD-95, GABA Receptors, CaMKIIα, and mGluR5 at Fiber Cell Membranes in the Eye Lens. Neurochem Res. 2015;40:2167-76 pubmed publisher
    ..that FMRP co-localizes at fiber cell membranes with PSD-95, GABAAδ, GABAAβ3, GABBR1, STEP, CaMKIIα, and mGluR5 in young adult lenses...
  7. Folsom T, Thuras P, Fatemi S. Protein expression of targets of the FMRP regulon is altered in brains of subjects with schizophrenia and mood disorders. Schizophr Res. 2015;165:201-11 pubmed publisher
    ..the fragile X mental retardation 1 (FMR1) gene leads to loss of expression of FMRP and upregulated metabotropic glutamate receptor 5 (mGluR5) signaling resulting in the multiple physical and cognitive deficits associated with fragile ..
  8. Sakai R, Swanson G, Shimamoto K, Green T, Contractor A, Ghetti A, et al. Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea. J Pharmacol Exp Ther. 2001;296:650-8 pubmed
    ..Surprisingly, in calcium imaging experiments we found that DH also activated recombinant mGluR5 receptors but did not activate mGluR1 receptors...
  9. Xu Y, Li Z, Yao L, Zhang X, Gan D, Jiang M, et al. Altered Norbin Expression in Patients with Epilepsy and a Rat Model. Sci Rep. 2017;7:13970 pubmed publisher
    ..Norbin is also an important endogenous modulator of metabotropic glutamate receptor 5 (mGluR5) signaling, and nervous system-specific homozygous gene disruptions, result in epileptic ..

More Information

Publications139 found, 100 shown here

  1. Banerjee A, Luong J, Ho A, Saib A, Ploski J. Overexpression of Homer1a in the basal and lateral amygdala impairs fear conditioning and induces an autism-like social impairment. Mol Autism. 2016;7:16 pubmed publisher
    ..are interesting in part because Homer1a influences the functioning of Shank3, metabotropic glutamate receptors (mGluR5), and Homer1, and these proteins have previously been associated with ASD, indicating that these differing models ..
  2. Seredynski A, Balthazart J, Ball G, Cornil C. Estrogen Receptor β Activation Rapidly Modulates Male Sexual Motivation through the Transactivation of Metabotropic Glutamate Receptor 1a. J Neurosci. 2015;35:13110-23 pubmed publisher
    ..The mGluR1a antagonist LY367385 significantly inhibited sexual motivation but mGluR2/3 and mGluR5 antagonists were ineffective...
  3. Kumar J, Hapidin H, Get Bee Y, Ismail Z. The effects of acute ethanol administration on ethanol withdrawal-induced anxiety-like syndrome in rats: A biochemical study. Alcohol. 2016;50:9-17 pubmed publisher
    ..Metabotropic glutamate receptor subtype 5 (mGlu5) and protein kinase C (PKC) epsilon have been reported to mediate acute and chronic effects of ethanol...
  4. Cozzoli D, Kaufman M, Nipper M, Hashimoto J, Wiren K, Finn D. Functional regulation of PI3K-associated signaling in the accumbens by binge alcohol drinking in male but not female mice. Neuropharmacology. 2016;105:164-174 pubmed publisher
    ..Binge alcohol intake decreased mGlu5 levels in females, whereas it decreased indices of phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin ..
  5. Liu M, Zhu Q, Wu J, Yu X, Hu M, Xie X, et al. Glutamate affects the production of epoxyeicosanoids within the brain: The up-regulation of brain CYP2J through the MAPK-CREB signaling pathway. Toxicology. 2017;381:31-38 pubmed publisher astrocytes in a dose-dependent manner, while an antagonist of the metabotropic glutamate receptor subtype 5 (mGlu5 receptor) attenuated the glutamate-induced increases in CYP2J2 levels by glutamate...
  6. Mantere O, Saarela M, Kieseppä T, Raij T, Mantyla T, Lindgren M, et al. Anti-neuronal anti-bodies in patients with early psychosis. Schizophr Res. 2018;192:404-407 pubmed publisher
    ..acid receptor (AMPA), glycine receptor (GlyR), metabotropic glutamate receptor 1 and 5 (mGluR1, mGluR5), anti-Tr/Delta/notch-like epidermal growth factor-related receptor (DNER), contactin-associated protein-like 2 (..
  7. O Riordan K, Huang I, Pizzi M, Spano P, Boroni F, Egli R, et al. Regulation of nuclear factor kappaB in the hippocampus by group I metabotropic glutamate receptors. J Neurosci. 2006;26:4870-9 pubmed
    ..An antagonist of mGluR5, 2-Methyl-6-(phenylethynyl)pyridine, inhibited the DHPG-induced activation of NF-kappaB, whereas an antagonist of ..
  8. Sun M, Hongpaisan J, Alkon D. Rescue of Synaptic Phenotypes and Spatial Memory in Young Fragile X Mice. J Pharmacol Exp Ther. 2016;357:300-10 pubmed publisher
    ..b>mGluR5 expression was in fact lower in fragile X mice and its expression was restored with the bryostatin-1 treatment...
  9. Gegelashvili G, Dehnes Y, Danbolt N, Schousboe A. The high-affinity glutamate transporters GLT1, GLAST, and EAAT4 are regulated via different signalling mechanisms. Neurochem Int. 2000;37:163-70 pubmed
    ..machinery for differential regulation of GLAST via the astroglial metabotropic glutamate receptors, mGluR3 and mGluR5. Thus, long-term treatment with the group I mGluR agonist, DHPG, causes down-regulation of GLAST, whereas the ..
  10. Stefanik M, Milovanovic M, Werner C, Spainhour J, Wolf M. Withdrawal From Cocaine Self-administration Alters the Regulation of Protein Translation in the Nucleus Accumbens. Biol Psychiatry. 2018;84:223-232 pubmed publisher
    ..We compared basal overall translation and its regulation by metabotropic glutamate receptor 1 (mGlu1), mGlu5, and N-methyl-D-aspartate receptors (NMDARs) in drug-naïve, saline control, and cocaine rats, and we compared ..
  11. Li C, Chai S, Ju Y, Hou L, Zhao H, Ma W, et al. Pu-erh Tea Protects the Nervous System by Inhibiting the Expression of Metabotropic Glutamate Receptor 5. Mol Neurobiol. 2017;54:5286-5299 pubmed publisher
    ..b>Metabotropic glutamate receptor 5 (mGluR5) is one of the glutamate receptors and represents a promising target for studying ..
  12. Manduca A, Bara A, Larrieu T, Lassalle O, Joffre C, Layé S, et al. Amplification of mGlu5-Endocannabinoid Signaling Rescues Behavioral and Synaptic Deficits in a Mouse Model of Adolescent and Adult Dietary Polyunsaturated Fatty Acid Imbalance. J Neurosci. 2017;37:6851-6868 pubmed publisher
    ..These findings have important implications for the identification of nutritional risk for disease and the design of new treatments for the behavioral deficits associated with nutritional n-3 PUFAs' imbalance. ..
  13. Reker A, Oliveros A, Sullivan J, Nahar L, Hinton D, Kim T, et al. Neurogranin in the nucleus accumbens regulates NMDA receptor tolerance and motivation for ethanol seeking. Neuropharmacology. 2018;131:58-67 pubmed publisher
    ..We identified that ethanol exposure decreases mGluR5 (metabotropic glutamate receptor 5) expression in the NAc of Ng-/- mice and pharmacological inhibition of mGluR5 reverses ..
  14. Loane D, Stoica B, Pajoohesh Ganji A, Byrnes K, Faden A. Activation of metabotropic glutamate receptor 5 modulates microglial reactivity and neurotoxicity by inhibiting NADPH oxidase. J Biol Chem. 2009;284:15629-39 pubmed publisher
    ..We demonstrate that the group I receptor member mGluR5 is highly expressed in primary microglial cultures and the BV2 microglial cell line...
  15. Lindemann L, Porter R, Scharf S, Kuennecke B, Bruns A, von Kienlin M, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015;353:213-33 pubmed publisher
    ..the treatment of MDD have increasingly received attention, and preclinical research suggests that metabotropic glutamate receptor 5 (mGlu5) inhibitors have antidepressant-like properties...
  16. Valero M, Caminos E, Juiz J, Martinez Galan J. TRPC1 and metabotropic glutamate receptor expression in rat auditory midbrain neurons. J Neurosci Res. 2015;93:964-72 pubmed publisher
    ..and Western blotting, this study assesses the presence of TRPC1 along with both group I mGluR subtypes mGluR1 and mGluR5 in the rat inferior colliculus (IC). All these molecules present a robust expression in the IC...
  17. Dąbrowska Bouta B, Strużyńska L, Chalimoniuk M, Frontczak Baniewicz M, Sulkowski G. The influence of glutamatergic receptor antagonists on biochemical and ultrastructural changes in myelin membranes of rats subjected to experimental autoimmune encephalomyelitis. Folia Neuropathol. 2015;53:317-26 pubmed
    ..amantadine and memantine (antagonists of NMDA receptors), LY 367384 (an antagonist of mGluR1), and MPEP (an mGluR5 antagonist) on the development of neurological symptoms in immunized animals, morphological changes in cerebral ..
  18. Hanak T, Libbey J, Doty D, Sim J, DePaula Silva A, Fujinami R. Positive modulation of mGluR5 attenuates seizures and reduces TNF-α+ macrophages and microglia in the brain in a murine model of virus-induced temporal lobe epilepsy. Exp Neurol. 2018;311:194-204 pubmed publisher
    ..The metabotropic glutamate receptor 5 (mGluR5) is a G-protein coupled receptor that has been shown to reduce IL-6 and TNF-α and to ..
  19. Palanisamy G, Marcek J, Cappon G, Whritenour J, Shaffer C, Brady J, et al. Drug-induced Skin Lesions in Cynomolgus Macaques Treated with Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulators. Toxicol Pathol. 2015;43:995-1003 pubmed publisher
    Three orally administered metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators caused skin lesions consistent with delayed type-IV hypersensitivity in cynomolgus macaques in 2- and 12-week toxicity studies...
  20. Sundararajan T, Manzardo A, Butler M. Functional analysis of schizophrenia genes using GeneAnalytics program and integrated databases. Gene. 2018;641:25-34 pubmed publisher
    ..g., GRIA1, GRIN2, GRIK4, GRM5), serotonergic receptors (e.g., HTR2A, HTR2C), GABAergic receptors (e.g...
  21. Wang W, Duclot F, Groveman B, Carrier N, Qiao H, Fang X, et al. Hippocampal protein kinase D1 is necessary for DHPG-induced learning and memory impairments in rats. PLoS ONE. 2018;13:e0195095 pubmed publisher
    ..Recent investigations have shown that the activation of group I mGluRs (mGluR1 and mGluR5) in cultured hippocampal neurons by application of (S)-3,5-Dihydroxyphenylglycine (DHPG) causes the regulated ..
  22. Blanco E, Pavón F, Palomino A, Luque Rojas M, Serrano A, Rivera P, et al. Cocaine-induced behavioral sensitization is associated with changes in the expression of endocannabinoid and glutamatergic signaling systems in the mouse prefrontal cortex. Int J Neuropsychopharmacol. 2014;18: pubmed publisher
    ..mice primed with cocaine, this inhibition was reversed and a strong increase was detected in the mGluR5, NR2 subunits, and both GluR1 and GluR3...
  23. Zimmermann J, Neuhuber W, Raab M. Homer1 (VesL-1) in the rat esophagus: focus on myenteric plexus and neuromuscular junction. Histochem Cell Biol. 2017;148:189-206 pubmed publisher
    ..Occurrence and location of Homer1 and mGluR5 in myenteric plexus and neuromuscular junctions (NMJ) of rat esophagus have yet not been characterized...
  24. An M, Kim C, Nam G, Kim D, Rhee S, Cho S, et al. Transcriptome analysis for UVB-induced phototoxicity in mouse retina. Environ Toxicol. 2018;33:52-62 pubmed publisher
    ..transcription factors (eg, Asxl2, Atf7, Per1, Phox2a, Rxra), RNA processing, and neuronal genes (eg, B4gal2, Drd1, Grm5, Rnf40, Rnps1, Usp39, Wbp4)...
  25. Yoshikawa K, Ohyama T, Takahashi E, Numajiri Y, Konno M, Moriyama M, et al. Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators. Bioorg Med Chem Lett. 2015;25:3135-41 pubmed publisher
    This Letter describes the identification of a series of novel non-acetylenic mGluR5 negative allosteric modulators based on the alpha-substituted acylamine structure...
  26. Kim S, Weon H, Youn D. Essential roles of mGluR1 and inhibitory synaptic transmission in NMDA-independent long-term potentiation in the spinal trigeminal interpolaris. Life Sci. 2016;144:54-60 pubmed publisher
    ..This LTP was not dependent on NMDA receptor activation; however, it did require the activation of mGluR1, but not mGluR5, and an intracellular Ca(2+) rise...
  27. Gawel K, Jenda Wojtanowska M, Gibula Bruzda E, Kedzierska E, Filarowska J, Marszalek Grabska M, et al. The influence of AMN082, metabotropic glutamate receptor 7 (mGlu7) allosteric agonist on the acute and chronic antinociceptive effects of morphine in the tail-immersion test in mice: Comparison with mGlu5 and mGlu2/3 ligands. Physiol Behav. 2018;185:112-120 pubmed publisher
    Preclinical data indicated that the metabotropic glutamate receptors 5 (mGlu5) and glutamate receptors 2/3 (mGlu2/3) are involved in modulating morphine antinociception...
  28. Daggett L, Sacaan A, Akong M, Rao S, Hess S, Liaw C, et al. Molecular and functional characterization of recombinant human metabotropic glutamate receptor subtype 5. Neuropharmacology. 1995;34:871-86 pubmed
    ..The distribution of mGluR5 mRNA in human brain was most strongly detected throughout the hippocampus, with moderate levels in the caudate-..
  29. Magen I, Torres E, Dinh D, Chung A, Masliah E, Chesselet M. Social Cognition Impairments in Mice Overexpressing Alpha-Synuclein Under the Thy1 Promoter, a Model of Pre-manifest Parkinson's Disease. J Parkinsons Dis. 2015;5:669-80 pubmed publisher
    ..have synaptic deficits in the frontostriatal pathway, low cortical acetylcholine, and high level of expression of mGluR5 receptors, which have all been implicated in social recognition deficits...
  30. Olde Loohuis N, Ba W, Stoerchel P, Kos A, Jager A, Schratt G, et al. MicroRNA-137 Controls AMPA-Receptor-Mediated Transmission and mGluR-Dependent LTD. Cell Rep. 2015;11:1876-84 pubmed publisher
    ..In addition, we find that miR-137 is transiently upregulated in response to metabotropic glutamate receptor 5 (mGluR5), but not mGluR1 activation...
  31. Shah F, Stepan A, O Mahony A, Velichko S, Folias A, Houle C, et al. Mechanisms of Skin Toxicity Associated with Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators. Cell Chem Biol. 2017;24:858-869.e5 pubmed publisher standardized panels of human primary cell/co-culture systems to characterize the skin toxicity mechanism(s) of mGluR5 NAMs from two different series...
  32. Piva A, Gerace E, Di Chio M, Osanni L, Padovani L, Caffino L, et al. The metaplastic effects of NMDA receptors blockade on reactivation of instrumental memories in rats. Neurobiol Learn Mem. 2018;154:87-96 pubmed publisher
    ..Vehicle/Retrieval group supported the behavioural findings. An increase of GluN2B, GluA1 and mGluR5 in NAc, and GluN2B in Amy, 24?h after MK-801 indicated the trigger of associated metaplastic changes...
  33. Dietz B, Manahan Vaughan D. Hippocampal long-term depression is facilitated by the acquisition and updating of memory of spatial auditory content and requires mGlu5 activation. Neuropharmacology. 2017;115:30-41 pubmed publisher
    ..reconfiguration of the same tones were both prevented by an antagonism of the metabotropic glutamate receptor, mGlu5. These data indicate that, if behaviourally salient enough, the hippocampus can use audiospatial cues to ..
  34. Haass Koffler C, Goodyear K, Long V, Tran H, Loche A, Cacciaglia R, et al. A Phase I randomized clinical trial testing the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative allosteric modulator GET 73 following single and repeated doses in healthy volunteers. Eur J Pharm Sci. 2017;109:78-85 pubmed publisher
    ..was to evaluate the safety, tolerability and pharmacokinetics (PK) of GET 73 (PubChem SID: 329974174), a novel mGluR5 negative allosteric modulator...
  35. Di Menna L, Joffe M, Iacovelli L, Orlando R, Lindsley C, Mairesse J, et al. Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system. Neuropharmacology. 2018;128:301-313 pubmed publisher
    b>mGlu5 receptors are involved in mechanisms of activity-dependent synaptic plasticity, and are targeted by drugs developed for the treatment of CNS disorders...
  36. Haass Koffler C, Goodyear K, Long V, Tran H, Loche A, Cacciaglia R, et al. Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters. Data Brief. 2017;15:407-413 pubmed publisher
    ..entitled "Phase I randomized clinical trial for the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative allosteric modulator GET 73 following single and repeated doses in healthy male volunteers" (Haass-..
  37. Ouattara B, Gregoire L, Morissette M, Gasparini F, Vranesic I, Bilbe G, et al. Metabotropic glutamate receptor type 5 in levodopa-induced motor complications. Neurobiol Aging. 2011;32:1286-95 pubmed publisher
    Metabotropic glutamate receptors type 5 (mGluR5) are implicated in regulation of synaptic plasticity and learning, and were the focus of our investigation in human Parkinson's disease (PD) patients with dyskinesias and wearing-off, and in ..
  38. Vanzulli I, Butt A. mGluR5 protect astrocytes from ischemic damage in postnatal CNS white matter. Cell Calcium. 2015;58:423-30 pubmed publisher
    ..Optic nerve astrocytes are shown to express mGluR5 using immunolabelling of sections and explant cultures from transgenic reporter mice in which GFAP drives ..
  39. Sengmany K, Gregory K. Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias. Br J Pharmacol. 2016;173:3001-17 pubmed publisher
    The metabotropic glutamate receptor subtype 5 (mGlu5 ) is a family C GPCR that has been implicated in various neuronal processes and, consequently, in several CNS disorders...
  40. Hullinger R, O Riordan K, Burger C. Environmental enrichment improves learning and memory and long-term potentiation in young adult rats through a mechanism requiring mGluR5 signaling and sustained activation of p70s6k. Neurobiol Learn Mem. 2015;125:126-34 pubmed publisher
    ..Our results demonstrate that this LTP is dependent on mGluR5 signaling, activation of ERK and mTOR signaling cascades, and sustained phosphorylation of p70s6 kinase, thus ..
  41. Yamasaki T, Fujinaga M, Kawamura K, Furutsuka K, Nengaki N, Shimoda Y, et al. Dynamic Changes in Striatal mGluR1 But Not mGluR5 during Pathological Progression of Parkinson's Disease in Human Alpha-Synuclein A53T Transgenic Rats: A Multi-PET Imaging Study. J Neurosci. 2016;36:375-84 pubmed publisher
    ..Group I metabotropic glutamate receptor subtypes 1 and 5 (mGluR1 and mGluR5, respectively) are important targets for investigation in several CNS disorders...
  42. Zhang X, Hu M, Zhang L, An J, Yan W, Zhang Z, et al. MTEP impedes the neuronal polarization and the activity of the Akt-NF-κB pathway in rat hippocampal neurons. J Neurosci Res. 2017;95:1730-1744 pubmed publisher
    b>Metabotropic glutamate receptor 5 (mGluR5) is extensively involved in neural survival, differentiation, dendritic morphology, synaptic plasticity, and neural circuit formation...
  43. Been L, Moore K, Kennedy B, Meisel R. Metabotropic Glutamate Receptor and Fragile X Signaling in a Female Model of Escalated Aggression. Biol Psychiatry. 2016;79:685-92 pubmed publisher
    ..Female hamsters were given five daily aggression tests with or without prior treatment with the metabotropic glutamate receptor 5 (mGluR5) antagonist 2-methyl-6-(phenylethynyl)-pyridine...
  44. Zolkowska D, Kondrat Wróbel M, Florek Luszczki M, Luszczki J. Influence of MPEP (a selective mGluR5 antagonist) on the anticonvulsant action of novel antiepileptic drugs against maximal electroshock-induced seizures in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2016;65:172-8 pubmed publisher
    ..2-methyl-6-(phenylethynyl)pyridine (MPEP - a selective antagonist for the glutamate metabotropic receptor subtype mGluR5) on the protective action of some novel antiepileptic drugs (lamotrigine, oxcarbazepine, pregabalin and topiramate)..
  45. Pitchers K, Di Sebastiano A, Coolen L. mGluR5 activation in the nucleus accumbens is not essential for sexual behavior or cross-sensitization of amphetamine responses by sexual experience. Neuropharmacology. 2016;107:122-130 pubmed publisher
    ..The latter is dependent on a period of abstinence from sexual reward. In this study, the role of mGluR5 activation in the NAc for expression of mating and the cross-sensitizing effects of sexual experience was tested...
  46. Travaglia A, Bisaz R, Sweet E, Blitzer R, Alberini C. Infantile amnesia reflects a developmental critical period for hippocampal learning. Nat Neurosci. 2016;19:1225-33 pubmed publisher
    ..receptor subunits from 2B to 2A, which is dependent on brain-derived neurotrophic factor (BDNF) and metabotropic glutamate receptor 5 (mGluR5). Activating BDNF or mGluR5 after training rescues the infantile amnesia...
  47. Javidan A, Taghizadeh M, Hosseini S, Iman M, Jafari R. Docking, Molecular Dynamics Simulation and Synthesis of New Fenobam Analogues as mGlu5 Receptor Antagonists. Comb Chem High Throughput Screen. 2016;19:764-770 pubmed
    Fenobam is a non-competitive mGluR5 antagonist as an anxiolytic agent. In this research a new series of fenobam analogues containing thiazole moiety instead of imidazole ring were designed and synthesized...
  48. Galambos J, Bielik A, Wágner G, Domány G, Kóti J, Béni Z, et al. Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators. Eur J Med Chem. 2017;133:240-254 pubmed publisher
    Negative allosteric modulators of metabotropic glutamate receptor 5 (mGlu5) showed efficacy in a number of animal models of different CNS diseases including anxiety and depression...
  49. Zhang D, Qi Y, Klyubin I, Ondrejcak T, Sarell C, Cuello A, et al. Targeting glutamatergic and cellular prion protein mechanisms of amyloid β-mediated persistent synaptic plasticity disruption: Longitudinal studies. Neuropharmacology. 2017;121:231-246 pubmed publisher
    ..a blood-based scavenging system, glutamate-oxaloacetate transaminase (GOT), and blocking metabotropic glutamate 5 (mGlu5) receptor or its co-receptor cellular prion protein (PrP), prevent the acute inhibition of long-term potentiation (..
  50. Sun H, Su R, Zhang X, Wen J, Yao D, Gao X, et al. Hippocampal GR- and CB1-mediated mGluR5 differentially produces susceptibility and resilience to acute and chronic mild stress in rats. Neuroscience. 2017;357:295-302 pubmed publisher
    ..The present study aimed to explore the relationship of metabotropic glutamate receptor 5 (mGluR5) with glucocorticoid receptor (GR) or cannabinoid receptor (CB1) and further indicate the ..
  51. Abdallah C, Hannestad J, Mason G, Holmes S, DellaGioia N, Sanacora G, et al. Metabotropic Glutamate Receptor 5 and Glutamate Involvement in Major Depressive Disorder: A Multimodal Imaging Study. Biol Psychiatry Cogn Neurosci Neuroimaging. 2017;2:449-456 pubmed publisher
    Preclinical and postmortem studies have implicated the metabotropic glutamate receptor 5 (mGluR5) in the pathophysiology of major depressive disorder (MDD)...
  52. O Riordan K, Hu N, Rowan M. Aß Facilitates LTD at Schaffer Collateral Synapses Preferentially in the Left Hippocampus. Cell Rep. 2018;22:2053-2065 pubmed publisher
    ..asymmetry, in the presence of Aß, the induction of LTD is preferentially enhanced in the left hippocampus in an mGluR5-dependent manner...
  53. Malosh C, Turlington M, Bridges T, Rook J, Noetzel M, Vinson P, et al. Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. Bioorg Med Chem Lett. 2015;25:5115-20 pubmed publisher
    We report the optimization of a series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from an acyl dihydropyrazolo[1,5-a]pyrimidinone class...
  54. Haas L, Salazar S, Kostylev M, Um J, Kaufman A, Strittmatter S. Metabotropic glutamate receptor 5 couples cellular prion protein to intracellular signalling in Alzheimer's disease. Brain. 2016;139:526-46 pubmed publisher
    ..disease-related phenotypes in mice can be rescued by blockade of either cellular prion protein or metabotropic glutamate receptor 5. We sought genetic and biochemical evidence that these proteins function cooperatively as an ..
  55. De Jesús Burgos M, González García S, Cruz Santa Y, Pérez Acevedo N. Amygdalar activation of group I metabotropic glutamate receptors produces anti- and pro-conflict effects depending upon animal sex in a sexually dimorphic conditioned conflict-based anxiety model. Behav Brain Res. 2016;302:200-12 pubmed publisher
    ..Western blot analyses showed that protein expression of mGluR1, but not mGluR5 was higher in OVX+EB>OVX>male rats in the amygdala, whereas no significant differences were detected in the ..
  56. Bhattacharyya S. Inside story of Group I Metabotropic Glutamate Receptors (mGluRs). Int J Biochem Cell Biol. 2016;77:205-12 pubmed publisher
    ..Among the eight subtypes, mGluR1 and mGluR5 belong to the group I family...
  57. Kim S, Hayashi H, Ishikawa T, Shibata K, Shigetomi E, Shinozaki Y, et al. Cortical astrocytes rewire somatosensory cortical circuits for peripheral neuropathic pain. J Clin Invest. 2016;126:1983-97 pubmed publisher
    ..of murine models, we have shown that sciatic nerve ligation induces a re-emergence of immature metabotropic glutamate receptor 5 (mGluR5) signaling in S1 astroglia, which elicits spontaneous somatic Ca2+ transients, synaptogenic ..
  58. Ade K, Wan Y, Hamann H, O Hare J, Guo W, Quian A, et al. Increased Metabotropic Glutamate Receptor 5 Signaling Underlies Obsessive-Compulsive Disorder-like Behavioral and Striatal Circuit Abnormalities in Mice. Biol Psychiatry. 2016;80:522-33 pubmed publisher
    ..Sapap3 knockout (KO) mice treated acutely with an mGluR5 antagonist were evaluated for OCD-relevant phenotypes of self-grooming, anxiety-like behaviors, and increased ..
  59. Heine J, Ly L, Lieker I, Slowinski T, Finke C, Prüss H, et al. Immunoadsorption or plasma exchange in the treatment of autoimmune encephalitis: a pilot study. J Neurol. 2016;263:2395-2402 pubmed
    ..and treatment effects of 21 patients with autoimmune encephalitis associated with NMDAR, LGI1, CASPR2, GAD, mGluR5 and Hu antibodies. Patients were randomly assigned to receive PE (n = 11) or IA (n = 10)...
  60. He Y, Li Y, Chen M, Pu Z, Zhang F, Chen L, et al. Habit Formation after Random Interval Training Is Associated with Increased Adenosine A2A Receptor and Dopamine D2 Receptor Heterodimers in the Striatum. Front Mol Neurosci. 2016;9:151 pubmed publisher
    ..interaction with the dopamine D2 receptors (D2Rs) and metabotropic glutamate receptors 5 (mGluR5) through receptor-receptor heterodimers, but in vivo evidence for these interactions is lacking...
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    ..However, the underlying mechanisms are largely unknown. We hypothesized that the alteration of metabotropic glutamate receptor 5 (mGluR5) in the brain region underlies such a comorbidity of aversive states...
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    Interaction between mGluR5 and NMDA receptors (NMDAR) is vital for synaptic plasticity and cognition...
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    ..neurotransmission and ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid/kainite (AMPA/KA) and metabotropic mGluR5 receptors is well established...
  64. Crabbé M, Van der Perren A, Weerasekera A, Himmelreich U, Baekelandt V, Van Laere K, et al. Altered mGluR5 binding potential and glutamine concentration in the 6-OHDA rat model of acute Parkinson's disease and levodopa-induced dyskinesia. Neurobiol Aging. 2018;61:82-92 pubmed publisher
    ..disease (PD) and levodopa-induced dyskinesia (LID), involving the metabotropic glutamate receptor type 5 (mGluR5)...
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    ..b>Metabotropic glutamate receptor 5 (mGluR5), for example, has been well documented to potentiate ionotropic NMDA receptor activity, ..
  66. Eng A, Kelver D, Hedrick T, Swanson G. Transduction of group I mGluR-mediated synaptic plasticity by ?-arrestin2 signalling. Nat Commun. 2016;7:13571 pubmed publisher
    Conventional signalling by the group I metabotropic glutamate receptors, mGluR1 and mGluR5, occurs through G-protein coupling, but evidence suggests they might also utilize other, non-canonical effector pathways...
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    ..This study shows that the metabotropic glutamate receptor, mGlu5, mobilizes nuclear Ca2+ independent of cytosolic Ca2+ regulation...
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    A feature of early postnatal neocortical development is a transient peak in signaling via metabotropic glutamate receptor 5 (mGluR5)...
  69. Felts A, Rodriguez A, Morrison R, Venable D, Blobaum A, Byers F, et al. N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. Bioorg Med Chem Lett. 2016;26:1894-900 pubmed publisher
    Selective negative allosteric modulators (NAMs) of each of the group I metabotropic glutamate receptors (mGlu1 and mGlu5) have been well characterized in the literature and offer potential as therapeutics in several disorders of the ..
  70. Gómez Santacana X, Dalton J, Rovira X, Pin J, Goudet C, Gorostiza P, et al. Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu5 negative allosteric modulation. Eur J Med Chem. 2017;127:567-576 pubmed publisher
    Modulation of metabotropic glutamate receptor 5 (mGlu5) with partial allosteric antagonists has received increased interest due to their favourable in vivo activity profiles compared to the unfavourable side-effects of full ..
  71. Gupta I, Young A. Metabotropic glutamate receptor modulation of dopamine release in the nucleus accumbens shell is unaffected by phencyclidine pretreatment: In vitro assessment using fast-scan cyclic voltammetry rat brain slices. Brain Res. 2018;1687:155-161 pubmed publisher
    ..pretreatment on modulation of dopamine neurotransmission by metabotropic glutamate receptors 2 and 5 (mGluR2 and mGluR5) in the nucleus accumbens shell in vitro, with the hypothesis that phencyclidine pretreatment would disrupt the ..
  72. Nasrallah C, Rottier K, Marcellin R, Compan V, Font J, Llebaria A, et al. Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci Rep. 2018;8:4407 pubmed publisher
    ..Our findings provide important mechanistic insights into mGlu5 G protein-dependent activity and selectivity. ..
  73. Kandratavicius L, Rosa Neto P, Monteiro M, Guiot M, Assirati J, Carlotti C, et al. Distinct increased metabotropic glutamate receptor type 5 (mGluR5) in temporal lobe epilepsy with and without hippocampal sclerosis. Hippocampus. 2013;23:1212-30 pubmed publisher
    Metabotropic glutamate receptor type 5 (mGluR5) upregulation in temporal lobe epilepsy (TLE) and the correlation of its expression with features of hippocampal sclerosis (HS) remains unclear...
  74. Chandley M, Szebeni A, Szebeni K, Crawford J, Stockmeier C, Turecki G, et al. Elevated gene expression of glutamate receptors in noradrenergic neurons from the locus coeruleus in major depression. Int J Neuropsychopharmacol. 2014;17:1569-78 pubmed publisher
    ..levels of the NMDA receptor subunit genes, GRIN2B and GRIN2C, and the metabotropic receptor genes, GRM4 and GRM5, in LC neurons...
  75. Mahato P, Pandey S, Bhattacharyya S. Differential effects of protein phosphatases in the recycling of metabotropic glutamate receptor 5. Neuroscience. 2015;306:138-50 pubmed publisher
    ..b>mGluR5, a member of the group I mGluR family is widely expressed throughout the brain and plays important roles in a ..
  76. Blacker C, Lewis C, Frye M, Veldic M. Metabotropic glutamate receptors as emerging research targets in bipolar disorder. Psychiatry Res. 2017;257:327-337 pubmed publisher
    ..X Mental Retardation Protein associated with altered mGluR1/5 activity in BD populations, and lithium decreasing mGluR5 expression and mGluR-mediated intracellular calcium signaling...
  77. Peterson C, Kitto K, Akgün E, Lunzer M, Riedl M, Vulchanova L, et al. Bivalent ligand that activates mu opioid receptor and antagonizes mGluR5 receptor reduces neuropathic pain in mice. Pain. 2017;158:2431-2441 pubmed publisher
    The mu opioid receptor (MOR) and metabotropic glutamate receptor 5 (mGluR5) are well-established pharmacological targets in the management of chronic pain. Both receptors are expressed in the spinal cord...
  78. Xie J, Chen S, Pan H. Presynaptic mGluR5 receptor controls glutamatergic input through protein kinase C-NMDA receptors in paclitaxel-induced neuropathic pain. J Biol Chem. 2017;292:20644-20654 pubmed publisher
    ..These effects were blocked by the selective mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP), but not by an mGluR1 antagonist...
  79. Boer K, Encha Razavi F, Sinico M, Aronica E. Differential distribution of group I metabotropic glutamate receptors in developing human cortex. Brain Res. 2010;1324:24-33 pubmed publisher, we have investigated the expression and cell-specific distribution of group I mGluRs (mGluR1alpha and mGluR5) during prenatal human cortical development...
  80. Price D, Rockenstein E, Ubhi K, Phung V, MacLean Lewis N, Askay D, et al. Alterations in mGluR5 expression and signaling in Lewy body disease and in transgenic models of alpha-synucleinopathy--implications for excitotoxicity. PLoS ONE. 2010;5:e14020 pubmed publisher
    ..accumulation of alpha-syn might result in alterations in metabotropic glutamate receptors (mGluR), particularly mGluR5 which has been linked to deficits in murine models of PD...
  81. Rohof W, Aronica E, Beaumont H, Troost D, Boeckxstaens G. Localization of mGluR5, GABAB, GABAA, and cannabinoid receptors on the vago-vagal reflex pathway responsible for transient lower esophageal sphincter relaxation in humans: an immunohistochemical study. Neurogastroenterol Motil. 2012;24:383-e173 pubmed publisher
    ..TLESRs are mediated by a vago-vagal reflex, which can be blocked by interaction with metabotropic Glutamate Receptor 5 (mGluR5), ?-aminobutyric acid type B (GABA(B)), ?-aminobutyric acid type A (GABA(A)), and ..
  82. Akkus F, Terbeck S, Ametamey S, Rufer M, Treyer V, Burger C, et al. Metabotropic glutamate receptor 5 binding in patients with obsessive-compulsive disorder. Int J Neuropsychopharmacol. 2014;17:1915-22 pubmed publisher
    ..magnetic resonance spectroscopy research points to glutamate dysfunction in OCD, we investigated the metabotropic glutamate receptor 5 (mGluR5) in patients with OCD and healthy controls...
  83. Chana G, Laskaris L, Pantelis C, Gillett P, Testa R, Zantomio D, et al. Decreased expression of mGluR5 within the dorsolateral prefrontal cortex in autism and increased microglial number in mGluR5 knockout mice: Pathophysiological and neurobehavioral implications. Brain Behav Immun. 2015;49:197-205 pubmed publisher
    b>Metabotropic glutamate receptor 5 (mGluR5) and microglial abnormalities have been implicated in autism spectrum disorder (ASD). However, controversy exists as to whether the receptor is down or upregulated in functioning in ASD...
  84. Ouachikh O, Chassain C, Pages G, Durif F, Hafidi A. mGlu5 receptor antagonist blocks bromocriptine-induced conditioned place preference in bilateral mesolimbic-lesioned rat. Behav Brain Res. 2017;317:301-310 pubmed publisher
    ..Therefore the potential implication of the metabotropic glutamate receptor 5 (mGluR5) antagonist (MTEP: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine) on bromocriptine-induced ..
  85. Lin S, Li X, Chen Y, Gao F, Chen H, Hu N, et al. Social Isolation During Adolescence Induces Anxiety Behaviors and Enhances Firing Activity in BLA Pyramidal Neurons via mGluR5 Upregulation. Mol Neurobiol. 2018;55:5310-5320 pubmed publisher
    ..and both intraperitoneal administration and intra-basolateral amygdala (BLA) infusion of MPEP, a metabotropic glutamate receptor 5 antagonist, normalized anxiety behaviors...
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    ..These observations support a model in which the dynamic expression of Homer 1a competes with constitutively expressed CC-Homers to modify synaptic mGluR properties. ..
  87. Kalariti N, Lembessis P, Papageorgiou E, Pissimissis N, Koutsilieris M. Regulation of the mGluR5, EAAT1 and GS expression by glucocorticoids in MG-63 osteoblast-like osteosarcoma cells. J Musculoskelet Neuronal Interact. 2007;7:113-8 pubmed
    ..We characterized the effects of dexamethasone on the expression of the mGluR5, EAAT1 and GS, at mRNA and protein level, using relative quantitative RTPCR and Western blot analysis, ..
  88. Fatemi S, Folsom T, Kneeland R, Liesch S. Metabotropic glutamate receptor 5 upregulation in children with autism is associated with underexpression of both Fragile X mental retardation protein and GABAA receptor beta 3 in adults with autism. Anat Rec (Hoboken). 2011;294:1635-45 pubmed publisher
    ..Additionally, we found that levels of metabotropic glutamate receptor 5 (mGluR5) protein were significantly increased in vermis of children with autism versus age and ..
  89. Vlot A, de Witte W, Danhof M, van der Graaf P, van Westen G, de Lange E. Target and Tissue Selectivity Prediction by Integrated Mechanistic Pharmacokinetic-Target Binding and Quantitative Structure Activity Modeling. AAPS J. 2017;20:11 pubmed publisher
    ..database are predicted by QSAR random forest (RF) modeling for the CB1 receptor and known off-targets (TRPV1, mGlu5, 5-HT1a)...
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    ..previously reported that a variant with extra amino acids exists in rat metabotropic glutamate receptor subtype 5 (mGluR5) and that the identical extra sequence also exists in the human mGluR5 cDNA...
  91. Brakeman P, Lanahan A, O Brien R, Roche K, Barnes C, Huganir R, et al. Homer: a protein that selectively binds metabotropic glutamate receptors. Nature. 1997;386:284-8 pubmed
    ..This dynamic transcriptional control suggests that Homer mediates a novel cellular mechanism that regulates metabotropic glutamate signalling. ..
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    ..activity has been observed for the glutamate GPCRs (the metabotropic glutamate receptors mGluR1a and mGluR5) when they are overexpressed in heterologous cells...