Gene Symbol: GRIK1
Description: glutamate ionotropic receptor kainate type subunit 1
Alias: EAA3, EEA3, GLR5, GLUR5, GluK1, gluR-5, glutamate receptor ionotropic, kainate 1, excitatory amino acid receptor 3, glutamate receptor 5
Species: human
Products:     GRIK1

Top Publications

  1. Bortolotto Z, Clarke V, Delany C, Parry M, Smolders I, Vignes M, et al. Kainate receptors are involved in synaptic plasticity. Nature. 1999;402:297-301 pubmed
    ..We find that LY382884 is a selective antagonist at neuronal kainate receptors containing the GluR5 subunit...
  2. Woo T, Shrestha K, Amstrong C, Minns M, Walsh J, Benes F. Differential alterations of kainate receptor subunits in inhibitory interneurons in the anterior cingulate cortex in schizophrenia and bipolar disorder. Schizophr Res. 2007;96:46-61 pubmed
    ..from schizophrenia, bipolar disorder, and normal control subjects, we simultaneously labeled the mRNA for the GluR5 or GluR6 subunit of the kainate receptor with [(35)S] and the mRNA for the 67 kD isoform of the GABA synthesizing ..
  3. 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
    ..DH displaced [3H]KA from recombinant GluR5 and GluR6 kainate receptor subunits expressed in HEK293 cells with K(i) values of 0.74 and 1.2 nM, respectively...
  4. Mennesson M, Rydgren E, Lipina T, Sokolowska E, Kulesskaya N, Morello F, et al. Kainate receptor auxiliary subunit NETO2 is required for normal fear expression and extinction. Neuropsychopharmacology. 2019;: pubmed publisher
    ..Variation in KAR genes has been associated with psychiatric disorders in humans, and in mice, knockouts of the Grik1 gene have increased, while Grik2 and Grik4 knockouts have reduced anxiety-like behavior...
  5. 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...
  6. 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...
  7. Hunter R, Bellani R, Bloss E, Costa A, McCarthy K, McEwen B. Regulation of kainate receptor subunit mRNA by stress and corticosteroids in the rat hippocampus. PLoS ONE. 2009;4:e4328 pubmed publisher
    ..of chronic stress and corticosteroid treatments upon the expression of the mRNA of kainate receptor subunits GluR5-7 and KA1-2...
  8. 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
    ..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 X ..
  9. Sherwood J, Amici M, Dargan S, Culley G, Fitzjohn S, Jane D, et al. Differences in kainate receptor involvement in hippocampal mossy fibre long-term potentiation depending on slice orientation. Neurochem Int. 2012;61:482-9 pubmed publisher
    ..We have reported previously that both frequency facilitation and LTP can be blocked by selective antagonism of GluK1 (formerly GluR5/Glu(K5))-containing KARs, but other groups have failed to reproduce this effect...

More Information

Publications133 found, 100 shown here

  1. 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 seizures...
  2. Kaneko J, Kanazawa N, Tominaga N, Kaneko A, Suga H, Usui R, et al. Practical issues in measuring autoantibodies to neuronal cell-surface antigens in autoimmune neurological disorders: 190 cases. J Neurol Sci. 2018;390:26-32 pubmed publisher
    ..receptor (GlyR) (n = 3), GABA(A) receptor (n = 2), GABA(B) receptor (n = 1), metabotrophic glutamate receptor 5 (n = 1), or unknown (n = 6); 3 had multiple NSA-antibodies...
  3. Dargan S, Clarke V, Alushin G, Sherwood J, Nisticò R, Bortolotto Z, et al. ACET is a highly potent and specific kainate receptor antagonist: characterisation and effects on hippocampal mossy fibre function. Neuropharmacology. 2009;56:121-30 pubmed publisher
    ..Here we used a highly potent and selective GluK1 (formerly GluR5) antagonist (ACET) to elucidate roles of GluK1-containing KARs in these synaptic processes...
  4. 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 NMDAR ..
  5. Dai J, Fu Y, Zeng Y, Li S, Qin Yin Z. Improved retinal function in RCS rats after suppressing the over-activation of mGluR5. Sci Rep. 2017;7:3546 pubmed publisher
    ..Following injection, the a-wave of the electroretinogram (ERG) was attenuated, and metabotropic glutamate receptor 5 (mGluR5) was activated...
  6. 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
    ..These data suggest that mGluR5 represents a novel target for modulating microglial-dependent neuroinflammation, and may have therapeutic relevance for neurological disorders that exhibit microglial-mediated neurodegeneration. ..
  7. Fatemi S, Folsom T, Liesch S, Kneeland R, Karkhane Yousefi M, Thuras P. The effects of prenatal H1N1 infection at E16 on FMRP, glutamate, GABA, and reelin signaling systems in developing murine cerebellum. J Neurosci Res. 2017;95:1110-1122 pubmed publisher gamma-aminobutyric acid, Reelin, and fragile X mental retardation protein (FMRP)-metabotropic glutamate receptor 5 signaling systems has also been demonstrated in these two disorders...
  8. Omiya Y, Uchigashima M, Konno K, Yamasaki M, Miyazaki T, Yoshida T, et al. VGluT3-expressing CCK-positive basket cells construct invaginating synapses enriched with endocannabinoid signaling proteins in particular cortical and cortex-like amygdaloid regions of mouse brains. J Neurosci. 2015;35:4215-28 pubmed publisher
  9. 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. 2019;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 provide ..
  10. Daroles L, Gribaudo S, Doulazmi M, Scotto Lomassese S, Dubacq C, Mandairon N, et al. Fragile X Mental Retardation Protein and Dendritic Local Translation of the Alpha Subunit of the Calcium/Calmodulin-Dependent Kinase II Messenger RNA Are Required for the Structural Plasticity Underlying Olfactory Learning. Biol Psychiatry. 2016;80:149-159 pubmed publisher
    ..neurons that are prevented by ablation of FMRP in adult-born neurons and rescued by an metabotropic glutamate receptor 5 antagonist...
  11. 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
    ..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...
  12. Abedi Z, Khaza Ai H, Vidyadaran S, Mutalib M. The Modulation of NMDA and AMPA/Kainate Receptors by Tocotrienol-Rich Fraction and ?-Tocopherol in Glutamate-Induced Injury of Primary Astrocytes. Biomedicines. 2017;5: pubmed publisher
    ..The expression levels of the ionotropic glutamate receptor genes (Gria2, Grin2A, GRIK1) were independently determined using RT-PCR...
  13. Kim K, Choi C, Kim J, Han S, Cheong J, Ryu J, et al. MeCP2 Modulates Sex Differences in the Postsynaptic Development of the Valproate Animal Model of Autism. Mol Neurobiol. 2016;53:40-56 pubmed publisher
    ..NMDAR), alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) and metabotropic glutamate receptor 5 (mGluR5) pathways in the prefrontal cortex of the VPA-exposed offspring at postnatal weeks 1, 2, and 4...
  14. Westmark P, Dekundy A, Gravius A, Danysz W, Westmark C. Rescue of Fmr1KO phenotypes with mGluR5 inhibitors: MRZ-8456 versus AFQ-056. Neurobiol Dis. 2018;119:190-198 pubmed publisher
    Metabotropic glutamate receptor 5 (mGluR5) is a drug target for central nervous system disorders such as fragile X syndrome that involve excessive glutamate-induced excitation...
  15. Areal L, Hamilton A, Martins Silva C, Pires R, Ferguson S. Neuronal scaffolding protein spinophilin is integral for cocaine-induced behavioral sensitization and ERK1/2 activation. Mol Brain. 2019;12:15 pubmed publisher
    ..1, and neuromodulatory G-protein coupled receptors, including dopamine receptor D2 and metabotropic glutamate receptor 5. Additionally, spinophilin is highly expressed in the striatum, a brain region that is fundamentally ..
  16. Kranzler H, WETHERILL R, Feinn R, Pond T, Gelernter J, Covault J. Posttreatment effects of topiramate treatment for heavy drinking. Alcohol Clin Exp Res. 2014;38:3017-23 pubmed publisher
    We examined whether the effects of topiramate and a single nucleotide polymorphism (rs2832407) in GRIK1, which encodes a kainate receptor subunit, persisted following a 12-week, placebo-controlled trial in 138 heavy drinkers with a ..
  17. Sun Y, Yang J, Hu X, Gao X, Li Y, Yu M, et al. Conditioned medium from overly excitatory primary astrocytes induced by La3+ increases apoptosis in primary neurons via upregulating the expression of NMDA receptors. Metallomics. 2018;10:1016-1028 pubmed publisher
    ..that LaCl3 treatment significantly upregulated the mRNA and protein expression levels of metabotropic glutamate receptor 5 (mGLUR5), phospholipase C (PLC), connexin 43 (Cx43) and Cx30, increased the concentrations of inositol ..
  18. Friend L, Weed J, Sandoval P, Nufer T, Ostlund I, Edwards J. CB1-Dependent Long-Term Depression in Ventral Tegmental Area GABA Neurons: A Novel Target for Marijuana. J Neurosci. 2017;37:10943-10954 pubmed publisher
    ..A novel CB1-dependent LTD was induced in GABA cells that was dependent on metabotropic glutamate receptor 5, and cannabinoid receptor 1 (CB1)...
  19. Lazzari C, Kipanyula M, Agostini M, Pozzan T, Fasolato C. Aβ42 oligomers selectively disrupt neuronal calcium release. Neurobiol Aging. 2015;36:877-85 pubmed publisher
    ..Ca(2+) dysregulation by Aβ42 oligomers involves metabotropic glutamate receptor 5 and requires network activity and the intact exo-endocytotic machinery, being prevented by tetrodotoxin and ..
  20. Lin T, Dang S, Su Q, Zhang H, Zhang J, Zhang L, et al. The Impact and Mechanism of Methylated Metabotropic Glutamate Receptors 1 and 5 in the Hippocampus on Depression-Like Behavior in Prenatal Stress Offspring Rats. J Clin Med. 2018;7: pubmed publisher to investigate the promoter methylation of metabotropic glutamate receptor 1 (mGluR1) and metabotropic Glutamate Receptor 5 (mGluR5) gene modification on PS induced depression-like behavior in offspring rats (OR)...
  21. Liang S, Alger B, McCarthy M. Developmental increase in hippocampal endocannabinoid mobilization: role of metabotropic glutamate receptor subtype 5 and phospholipase C. J Neurophysiol. 2014;112:2605-15 pubmed publisher
    ..Western blotting revealed significant increases in both metabotropic type glutamate receptor 5 (mGluR5) and PLCβ1 proteins in juveniles compared with neonates...
  22. Provenzano G, Sgadò P, Genovesi S, Zunino G, Casarosa S, Bozzi Y. Hippocampal dysregulation of FMRP/mGluR5 signaling in engrailed-2 knockout mice: a model of autism spectrum disorders. Neuroreport. 2015;26:1101-5 pubmed publisher
    ..Dysfunctions in fragile X mental retardation protein (FMRP), metabotropic glutamate receptor 5 (mGluR5), and GABAergic signaling pathways have been proposed as a possible pathogenic mechanism of autism ..
  23. Aseervatham G, Suryakala U, Doulethunisha -, Sundaram S, Bose P, Sivasudha T. Expression pattern of NMDA receptors reveals antiepileptic potential of apigenin 8-C-glucoside and chlorogenic acid in pilocarpine induced epileptic mice. Biomed Pharmacother. 2016;82:54-64 pubmed publisher
    ..05) inhibited by AP8CG and CA in a lower dose. The mRNA expression of GRIK1 did not differ significantly in any of the group and showed a similar pattern of expression...
  24. Elmenhorst D, Mertens K, Kroll T, Oskamp A, Ermert J, Elmenhorst E, et al. Circadian variation of metabotropic glutamate receptor 5 availability in the rat brain. J Sleep Res. 2016;25:754-761 pubmed publisher
    ..Given that altered mGluR5 densities play a role in psychiatric disorders, further investigation is warranted to evaluate their circadian involvement in mood changes in humans. ..
  25. Lee K, Westin L, Kim J, Chang J, Oh Y, Amreen B, et al. Alteration by p11 of mGluR5 localization regulates depression-like behaviors. Mol Psychiatry. 2015;20:1546-56 pubmed publisher
    ..p11 directly binds to the cytoplasmic tail of metabotropic glutamate receptor 5 (mGluR5)...
  26. Berry Kravis E, des Portes V, Hagerman R, Jacquemont S, Charles P, Visootsak J, et al. Mavoglurant in fragile X syndrome: Results of two randomized, double-blind, placebo-controlled trials. Sci Transl Med. 2016;8:321ra5 pubmed publisher animal models has described altered synaptic plasticity, a result of the up-regulation of metabotropic glutamate receptor 5 (mGluR5)-mediated signaling, as a putative downstream effect...
  27. Huang C, Liang Y, Lee C, Hsu K. Cocaine Withdrawal Impairs mGluR5-Dependent Long-Term Depression in Nucleus Accumbens Shell Neurons of Both Direct and Indirect Pathways. Mol Neurobiol. 2015;52:1223-1233 pubmed publisher
    ..from repeated cocaine exposure exhibited a selective deficit in the ability to elicit metabotropic glutamate receptor 5 (mGluR5)-dependent long-term depression (LTD) in the nucleus accumbens (NAc) shell...
  28. Feng L, Fernandez Martinez J, Zaal K, deAndrés Galiana E, Wolff B, Saligan L. mGluR5 mediates post-radiotherapy fatigue development in cancer patients. Transl Psychiatry. 2018;8:110 pubmed publisher
    ..1. Cells were pretreated with metabotropic glutamate receptor 5 (mGluR5) agonist (DHPG), antagonist (MPEP), or control (PBS) for 20 min before irradiation at 8 Gy in a ..
  29. Liu B, Zhao S, Qi C, Zhao X, Liu B, Hao F, et al. Inhibition of metabotropic glutamate receptor 5 facilitates hypoxia-induced glioma cell death. Brain Res. 2019;1704:241-248 pubmed publisher
    ..Akt activation reversed mGluR5 inhibition on hypoxia-induced glioma cell death. These results suggest mGluR5 as a potential therapeutic target for hypoxic tumors such as malignant glioma. ..
  30. Jane D, Lodge D, Collingridge G. Kainate receptors: pharmacology, function and therapeutic potential. Neuropharmacology. 2009;56:90-113 pubmed publisher
    ..g. LY382884 and ACET) and allosteric antagonists for KARs that contain GluK1 (GluR5) subunits have been developed. However, no selective ligands for the other KAR subunits have been identified...
  31. Qin M, Huang T, Kader M, Krych L, Xia Z, Burlin T, et al. R-Baclofen Reverses a Social Behavior Deficit and Elevated Protein Synthesis in a Mouse Model of Fragile X Syndrome. Int J Neuropsychopharmacol. 2015;18: pubmed publisher
    ..Ninety min after R-baclofen treatment, we observed an increase in metabotropic glutamate receptor 5 expression in the frontal cortex, a finding that may shed light on the tolerance observed in human studies ..
  32. Cao L, Tian Y, Jiang Y, Zhang G, Lei H, DI Z. Down-regulation of Homer1b/c protects against chemically induced seizures through inhibition of mTOR signaling. Cell Physiol Biochem. 2015;35:1633-42 pubmed publisher
    ..Homer1b/c knockdown-induced inhibition of mTOR pathway was partially ablated by the metabotropic glutamate receptor 5 (mGluR5) agonist CHPG...
  33. Gogliotti R, Senter R, Rook J, Ghoshal A, Zamorano R, Malosh C, et al. mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome. Hum Mol Genet. 2016;25:1990-2004 pubmed
    ..We report that expression of a key regulator of synaptic protein synthesis, the metabotropic glutamate receptor 5 (mGlu5) protein, is significantly reduced in both the brains of RS model mice and in the motor ..
  34. Arias H, Ravazzini F, Targowska Duda K, Kaczor A, Feuerbach D, Boffi J, et al. Positive allosteric modulators of ?7 nicotinic acetylcholine receptors affect neither the function of other ligand- and voltage-gated ion channels and acetylcholinesterase, nor ?-amyloid content. Int J Biochem Cell Biol. 2016;76:19-30 pubmed publisher
    ..PAM-2 affects neither the activity of m5-HT3ARs, GluR5/KA2 (a kainate-sensitive GluR), nor AChE, and PAM-4 does not affect agonist-activated r?9?10 AChRs...
  35. Zhang Y, Venkitaramani D, Gladding C, Zhang Y, Kurup P, Molnar E, et al. The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation. J Neurosci. 2008;28:10561-6 pubmed publisher hippocampal slices and synaptoneurosomes, a process that requires stimulation of mGluR5 (metabotropic glutamate receptor 5) and activation of mitogen-activated protein kinases and phosphoinositide-3 kinase pathways...
  36. Balu D, Li Y, Takagi S, Presti K, Ramikie T, Rook J, et al. An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia. Neuropsychopharmacology. 2016;41:2052-61 pubmed publisher
    ..Metabotropic glutamate receptor 5 (mGlu5)-positive allosteric modulators (PAMs) are currently being developed to treat cognitive dysfunction...
  37. Beraldo F, Ostapchenko V, Caetano F, Guimarães A, Ferretti G, Daude N, et al. Regulation of Amyloid ? Oligomer Binding to Neurons and Neurotoxicity by the Prion Protein-mGluR5 Complex. J Biol Chem. 2016;291:21945-21955 pubmed
    ..PrPC, laminin, and metabotropic glutamate receptor 5 (mGluR5) form a protein complex on the plasma membrane that can trigger signaling pathways involved in ..
  38. Eubanks J, Puranam R, Kleckner N, Bettler B, Heinemann S, McNamara J. The gene encoding the glutamate receptor subunit GluR5 is located on human chromosome 21q21.1-22.1 in the vicinity of the gene for familial amyotrophic lateral sclerosis. Proc Natl Acad Sci U S A. 1993;90:178-82 pubmed
    Genomic clones of the human non-N-methyl-D-aspartate (non-NMDA) glutamate receptor subunit GluR5 were isolated by high-stringency screening of a cosmid library using the rat cDNA as a probe...
  39. Kranzler H, Armeli S, Feinn R, Tennen H, Gelernter J, Covault J. GRIK1 genotype moderates topiramate's effects on daily drinking level, expectations of alcohol's positive effects and desire to drink. Int J Neuropsychopharmacol. 2014;17:1549-56 pubmed publisher the intent-to-treat effects of topiramate, we found that a single nucleotide polymorphism (rs2832407) in GRIK1, encoding the GluK1 subunit of the kainate receptor, moderated the treatment effect in European Americans (EAs; n ..
  40. Kouvaros S, Papatheodoropoulos C. Major dorsoventral differences in the modulation of the local CA1 hippocampal network by NMDA, mGlu5, adenosine A2A and cannabinoid CB1 receptors. Neuroscience. 2016;317:47-64 pubmed publisher
    ..We propose that the higher modulatory role of A2AR and mGluR5, in combination with the role of CB1Rs, provide DH with higher functional flexibility of its NMDARs, compared with VH. ..
  41. Zanos P, Georgiou P, Gonzalez L, Hourani S, Chen Y, Kitchen I, et al. Emotional Impairment and Persistent Upregulation of mGlu5 Receptor following Morphine Abstinence: Implications of an mGlu5-MOPr Interaction. Int J Neuropsychopharmacol. 2016;19: pubmed publisher
    ..Several lines of evidence suggest a role for the metabotropic glutamate receptor 5 in opioid addiction; however, its involvement during opioid withdrawal is not clear...
  42. Zurawek D, Salerno Kochan A, Dziedzicka Wasylewska M, Nikiforuk A, Kos T, Popik P. Changes in the expression of metabotropic glutamate receptor 5 (mGluR5) in a ketamine-based animal model of schizophrenia. Schizophr Res. 2018;192:423-430 pubmed publisher
    ..We postulate that increased expression of mGluR5 receptors in the dorsal part of the hippocampus may reflect compensatory changes to imbalanced glutamate neurotransmission associated with the hypoactivation of NMDA receptors. ..
  43. Sethna F, Wang H. Acute inhibition of mGluR5 disrupts behavioral flexibility. Neurobiol Learn Mem. 2016;130:1-6 pubmed publisher
    ..Intraperitoneal injection of the mGluR5 (metabotropic glutamate receptor 5) antagonist MPEP [2-Methyl-6-(phenylethynyl) pyridine hydrochloride] allowed the retrieval but prevented ..
  44. Selvam C, Thilagavathi R, Narasimhan B, Kumar P, Jordan B, Ranganna K. Computer-aided design of negative allosteric modulators of metabotropic glutamate receptor 5 (mGluR5): Comparative molecular field analysis of aryl ether derivatives. Bioorg Med Chem Lett. 2016;26:1140-4 pubmed publisher
    ..The study produced a statistically significant model with high correlation coefficient and good predictive abilities. ..
  45. Sander T, Hildmann T, Kretz R, Furst R, Sailer U, Bauer G, et al. Allelic association of juvenile absence epilepsy with a GluR5 kainate receptor gene (GRIK1) polymorphism. Am J Med Genet. 1997;74:416-21 pubmed
    ..A tetranucleotide repeat polymorphism in the non-coding region of the kainate-selective GluR5 receptor gene (GRIK1) on chromosome 21q22.1 provides the tool to investigate this candidate gene...
  46. Buscemi L, Ginet V, Lopatár J, Montana V, Pucci L, Spagnuolo P, et al. Homer1 Scaffold Proteins Govern Ca2+ Dynamics in Normal and Reactive Astrocytes. Cereb Cortex. 2017;27:2365-2384 pubmed publisher
    In astrocytes, the intracellular calcium (Ca2+) signaling mediated by activation of metabotropic glutamate receptor 5 (mGlu5) is crucially involved in the modulation of many aspects of brain physiology, including gliotransmission...
  47. Sengmany K, Singh J, Stewart G, Conn P, Christopoulos A, Gregory K. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017;115:60-72 pubmed publisher
    ..This article is part of the Special Issue entitled 'Metabotropic Glutamate Receptors, 5 years on'. ..
  48. Dominguez E, Iyengar S, Shannon H, Bleakman D, Alt A, Arnold B, et al. Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. J Med Chem. 2005;48:4200-3 pubmed
    Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors...
  49. Kuribayashi N, Uchida D, Kinouchi M, Takamaru N, Tamatani T, Nagai H, et al. The role of metabotropic glutamate receptor 5 on the stromal cell-derived factor-1/CXCR4 system in oral cancer. PLoS ONE. 2013;8:e80773 pubmed publisher
    ..We identified a gene that is highly upregulated in B88-SDF-1 cells, metabotropic glutamate receptor 5 (mGluR5), which was downregulated following treatment with 1,1' -[1,4-Phenylenebis(methylene)]bis-1,4,8,11-..
  50. Mao L, Wang J. Dopamine D2 receptors are involved in the regulation of Fyn and metabotropic glutamate receptor 5 phosphorylation in the rat striatum in vivo. J Neurosci Res. 2016;94:329-38 pubmed publisher
    ..Moreover, we explore whether D2Rs regulate metabotropic glutamate receptor 5 (mGluR5) in its tyrosine phosphorylation and whether the D2R-SFK pathway modulates trafficking of mGluR5...
  51. Kiritoshi T, Ji G, Neugebauer V. Rescue of Impaired mGluR5-Driven Endocannabinoid Signaling Restores Prefrontal Cortical Output to Inhibit Pain in Arthritic Rats. J Neurosci. 2016;36:837-50 pubmed publisher
    ..Underlying mechanisms remain to be determined. Here we advance the novel concept that metabotropic glutamate receptor 5 (mGluR5) fails to engage endocannabinoid (2-AG) signaling to overcome abnormal synaptic inhibition in pain, ..
  52. Bai X, Gu L, Yang H, Xi S, Xia N, Zhang S, et al. Downregulation of metabotropic glutamate receptor 5 inhibits hepatoma development in a neurotoxin rotenone-induced Parkinson's disease model. Toxicol Lett. 2018;288:71-81 pubmed publisher
    ..In our study, the effect of metabotropic glutamate receptor 5 (mGlu5) on hepatoma was explored in a rotenone-induced PD model both in vitro and in vivo...
  53. de Laat B, Leurquin Sterk G, Celen S, Bormans G, Koole M, Van Laere K, et al. Preclinical Evaluation and Quantification of 18F-FPEB as a Radioligand for PET Imaging of the Metabotropic Glutamate Receptor 5. J Nucl Med. 2015;56:1954-9 pubmed publisher
    The metabotropic glutamate receptor 5 (mGluR5) is a high-interest target for PET imaging because it plays a role in several pathologies, including addiction, schizophrenia, and fragile X syndrome...
  54. Tison F, Keywood C, Wakefield M, Durif F, Corvol J, Eggert K, et al. A Phase 2A Trial of the Novel mGluR5-Negative Allosteric Modulator Dipraglurant for Levodopa-Induced Dyskinesia in Parkinson's Disease. Mov Disord. 2016;31:1373-80 pubmed publisher
    The metabotropic glutamate receptor 5-negative allosteric modulator dipraglurant reduces levodopa-induced dyskinesia in the MPTP-macaque model...
  55. Batista E, Doria J, Ferreira Vieira T, Alves Silva J, Ferguson S, Moreira F, et al. Orchestrated activation of mGluR5 and CB1 promotes neuroprotection. Mol Brain. 2016;9:80 pubmed publisher
    The metabotropic glutamate receptor 5 (mGluR5) and the cannabinoid receptor 1 (CB1) exhibit a functional interaction, as CB1 regulates pre-synaptic glutamate release and mGluR5 activation increases endocannabinoid synthesis at the post-..
  56. Holmes S, Girgenti M, Davis M, Pietrzak R, DellaGioia N, Nabulsi N, et al. Altered metabotropic glutamate receptor 5 markers in PTSD: In vivo and postmortem evidence. Proc Natl Acad Sci U S A. 2017;114:8390-8395 pubmed publisher
    ..Specifically, the metabotropic glutamate receptor 5 (mGluR5) represents a promising treatment target...
  57. Marszalek Grabska M, Gibula Bruzda E, Bodzon Kulakowska A, Suder P, Gawel K, Filarowska J, et al. Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Impairment of Novel Object Recognition Induced by Acute Ethanol and Ethanol Withdrawal in Rats. Neurotox Res. 2018;33:607-620 pubmed publisher
    ..Moreover, mGlu5 (hippocampus, prefrontal cortex, and striatum) and mGlu2 (hippocampus) receptors play an important role in the ethanol-induced recognition memory impairment induced by ethanol withdrawal. ..
  58. Docherty S, Kovas Y, Plomin R. Gene-environment interaction in the etiology of mathematical ability using SNP sets. Behav Genet. 2011;41:141-54 pubmed publisher
  59. Marton T, Hussain Shuler M, Worley P. Homer 1a and mGluR5 phosphorylation in reward-sensitive metaplasticity: A hypothesis of neuronal selection and bidirectional synaptic plasticity. Brain Res. 2015;1628:17-28 pubmed publisher
    ..mechanism involving the induction of the immediate early gene Homer 1a, the phosphorylation of metabotropic glutamate receptor 5 (mGluR5)'s Homer ligand, and the enhancement of an NMDA receptor-dependent current...
  60. Zhang Z, Hu F, Ma B, Chen X, Zhu K, Shi Y, et al. Activation of type 5 metabotropic glutamate receptor promotes the proliferation of rat retinal progenitor cell via activation of the PI-3-K and MAPK signaling pathways. Neuroscience. 2016;322:138-51 pubmed publisher
    The metabotropic glutamate receptor 5 (mGluR5) regulates neurogenesis in the brain, but the effect of mGluR5 on retinal progenitor cells (RPCs) remains unknown...
  61. Luoni A, Gass P, Brambilla P, Ruggeri M, Riva M, Inta D. Altered expression of schizophrenia-related genes in mice lacking mGlu5 receptors. Eur Arch Psychiatry Clin Neurosci. 2018;268:77-87 pubmed publisher
    ..the hippocampus and prefrontal/frontal cortex (PFC/FC) of mice with a genetic deletion of the metabotropic glutamate receptor 5 (mGlu5), addressing key components of the GABAergic and glutamatergic systems...
  62. López Zapata A, León Navarro D, Crespo M, Albasanz J, Martín M. Chronic oral administration of MPEP, an antagonist of mGlu5 receptor, during gestation and lactation alters mGlu5 and A2A receptors in maternal and neonatal brain. Neuroscience. 2017;344:187-203 pubmed publisher
    ..The metabotropic glutamate receptor 5 (mGlu5) antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) exerts antidepressant- and ..
  63. 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
    ..Metabotropic glutamate receptor 5 (mGluR5) is one of the glutamate receptors and represents a promising target for studying neuroprotective ..
  64. Isherwood S, Pekcec A, Nicholson J, Robbins T, Dalley J. Dissociable effects of mGluR5 allosteric modulation on distinct forms of impulsivity in rats: interaction with NMDA receptor antagonism. Psychopharmacology (Berl). 2015;232:3327-44 pubmed publisher
    ..Although synergistic interactions exist between NMDA receptors and metabotropic glutamate receptor 5 (mGluR5), the significance of this interaction for impulsivity is unknown...
  65. Lee W, Parpura V. Spatio-temporal characteristics of metabotropic glutamate receptor 5 traffic at or near the plasma membrane in astrocytes. Glia. 2016;64:1050-65 pubmed publisher
    ..their intracellular Ca(2+) levels via the activation of G-protein coupled receptors, such as metabotropic glutamate receptor 5 (mGluR5), which, during early postnatal development, is the primary receptor responsible for glutamatergic ..
  66. Suryavanshi P, Gupta S, Yadav R, Kesherwani V, Liu J, Dravid S. Glutamate Delta-1 Receptor Regulates Metabotropic Glutamate Receptor 5 Signaling in the Hippocampus. Mol Pharmacol. 2016;90:96-105 pubmed publisher
    ..Here, we identified a novel role of GluD1 in regulating metabotropic glutamate receptor 5 (mGlu5) signaling in the hippocampus...
  67. Xi S, Bai X, Gu L, Bao L, Yang H, An W, et al. Metabotropic glutamate receptor 5 mediates the suppressive effect of 6-OHDA-induced model of Parkinson's disease on liver cancer. Pharmacol Res. 2017;121:145-157 pubmed publisher
    ..However, the underlying mechanisms remain unclear. In the present study, the role of metabotropic glutamate receptor 5 (mGluR5) has been investigated in 6-hydroxydopamine (6-OHDA)-induced PD combined with liver cancer both in ..
  68. Abd Elrahman K, Hamilton A, Hutchinson S, Liu F, Russell R, Ferguson S. mGluR5 antagonism increases autophagy and prevents disease progression in the zQ175 mouse model of Huntington's disease. Sci Signal. 2017;10: pubmed publisher
    ..huntingtin knockin mice for 12 weeks with CTEP, a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), reduced the size and number of huntingtin aggregates, attenuated caspase-3 activity, and reduced ..
  69. Gregor P, O Hara B, Yang X, Uhl G. Expression and novel subunit isoforms of glutamate receptor genes GluR5 and GluR6. Neuroreport. 1993;4:1343-6 pubmed
    Molecular heterogeneity of kainate-selective glutamate receptor subunits GluR5 and GluR6 was revealed by identification of a human cDNA, GluR5-1d, and a murine cDNA, GluR6-2, that each encode subunits with novel carboxy-terminal ..
  70. Arsenault D, Coulombe K, Zhu A, Gong C, Kil K, Choi J, et al. Loss of Metabotropic Glutamate Receptor 5 Function on Peripheral Benzodiazepine Receptor in Mice Prenatally Exposed to LPS. PLoS ONE. 2015;10:e0142093 pubmed publisher
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    b>GluK1 is a kainate receptor subunit in the ionotropic glutamate receptor family and can form functional channels when expressed, for instance, in HEK-293 cells. However, the channel-opening mechanism of GluK1 is poorly understood...
  72. Ghosh D, Gochhait S, Banerjee D, Chatterjee A, Sinha S, Nandagopal K. SNaPshot Assay in Quantitative Detection of Allelic Nondisjunction in Down Syndrome. Genet Test Mol Biomarkers. 2012;16:1226-35 pubmed publisher
    ..Since the GRIK1 and GARS-AIRS-GART genes, mapping to chromosome 21q22...
  73. Kranzler H, Feinn R, Gelernter J, Pond T, Covault J. Topiramate's reduction of body mass index in heavy drinkers: lack of moderation by a GRIK1 polymorphism. Exp Clin Psychopharmacol. 2014;22:419-23 pubmed publisher
    ..Further, in the European American (EA) subsample (n = 122), a single nucleotide polymorphism (rs2832407) in GRIK1, which encodes the GluK1 subunit of the kainate receptor, moderated the effect on heavy drinking days...
  74. Zarnadze S, Bauerle P, Santos Torres J, Böhm C, Schmitz D, Geiger J, et al. Cell-specific synaptic plasticity induced by network oscillations. elife. 2016;5: pubmed publisher
    ..Thus, we propose that gamma frequency oscillations represent a network state that introduces long-lasting synaptic plasticity in a cell-specific manner. ..
  75. Ragia G, Veresies I, Veresie L, Veresies K, Manolopoulos V. Association study of DRD2 A2/A1, DRD3 Ser9Gly, DβH -1021C>T, OPRM1 A118G and GRIK1 rs2832407C>A polymorphisms with alcohol dependence. Drug Metab Pers Ther. 2016;31:143-50 pubmed publisher
    ..Genes of dopaminergic (DRD2, DRD3 and DβH), opioid (OPRM1) and glutaminergic (GRIK1) systems mediate the dependent behavior via different mechanisms; however, they all target the serotonergic and ..
  76. 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 ..
  77. Stansley B, Fisher N, Gogliotti R, Lindsley C, Conn P, Niswender C. Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5. Cereb Cortex. 2017;:1-14 pubmed publisher
    ..These findings suggest that mGlu5-dependent metaplasticity within the hippocampus may play a critical role in extinction of contextual fear...
  78. Warnock G, Sommerauer M, Mu L, Pla Gonzalez G, Geistlich S, Treyer V, et al. A first-in-man PET study of [18F]PSS232, a fluorinated ABP688 derivative for imaging metabotropic glutamate receptor subtype 5. Eur J Nucl Med Mol Imaging. 2018;45:1041-1051 pubmed publisher
    Non-invasive imaging of metabotropic glutamate receptor 5 (mGlu5) in the brain using PET is of interest in e.g., anxiety, depression, and Parkinson's disease...
  79. Kelly E, Schaeffer S, Dhamne S, Lipton J, Lindemann L, Honer M, et al. mGluR5 Modulation of Behavioral and Epileptic Phenotypes in a Mouse Model of Tuberous Sclerosis Complex. Neuropsychopharmacology. 2017;: pubmed publisher
    Drugs targeting metabotropic glutamate receptor 5 (mGluR5) have therapeutic potential in autism spectrum disorders (ASD), including Tuberous Sclerosis Complex (TSC)...
  80. Korczak B, Nutt S, Fletcher E, Hoo K, Elliott C, Rampersad V, et al. cDNA cloning and functional properties of human glutamate receptor EAA3 (GluR5) in homomeric and heteromeric configuration. Receptors Channels. 1995;3:41-9 pubmed
    ..This cDNA clone, designated EAA3a, shares a 90% nucleotide identity with the previously reported rat GluR5-2b cDNA splice variant and differed from human GluR5-1d in the amino and carboxy terminal regions...
  81. Moriyoshi K, Iijima K, Fujii H, Ito H, Cho Y, Nakanishi S. Seven in absentia homolog 1A mediates ubiquitination and degradation of group 1 metabotropic glutamate receptors. Proc Natl Acad Sci U S A. 2004;101:8614-9 pubmed
  82. Li J, Zeng Y, Peng F, Li L, Yang T, Hong Z, et al. Aberrant glutamate receptor 5 expression in temporal lobe epilepsy lesions. Brain Res. 2010;1311:166-74 pubmed publisher
    b>Glutamate receptor 5 (GluR5) plays a role as an excitatory regulator of synaptic transmission and plasticity; however, its exact role in the pathological mechanism underlying epilepsy is not fully known...
  83. Giegling I, Drago A, Dolzan V, Plesnicar B, Schafer M, Hartmann A, et al. Glutamatergic gene variants impact the clinical profile of efficacy and side effects of haloperidol. Pharmacogenet Genomics. 2011;21:206-16 pubmed publisher
    ..set of 62 SNPs located in genes coding for subunits of glutamatergic receptors (GAD1, GRIA1, GRIA3, GRIA4, GRID2, GRIK1, GRIK2, GRIK3, GRIK4, GRIN2B, GRM1 and GRM4), and the transporter of glycine (SLC6A5), as modulators of the ..
  84. Bach P, Kirsch M, Hoffmann S, Jorde A, Mann K, Frank J, et al. The effects of single nucleotide polymorphisms in glutamatergic neurotransmission genes on neural response to alcohol cues and craving. Addict Biol. 2015;20:1022-32 pubmed publisher
    ..SNPs) in the genes of the N-Methyl-d-aspartate receptor (GRIN1, GRIN2A, GRIN2C) and kainate receptor (GRIK1), which have been previously associated with alcoholism, on behavior, neural cue-reactivity and drinking outcome...
  85. Khariv V, Ni L, Ratnayake A, Sampath S, Lutz B, Tao X, et al. Impaired sensitivity to pain stimuli in plasma membrane calcium ATPase 2 (PMCA2) heterozygous mice: a possible modality- and sex-specific role for PMCA2 in nociception. FASEB J. 2017;31:224-237 pubmed publisher
    ..acid receptor subunit GluR1, GABABR1, and GABABR2 levels, whereas metabotropic glutamate receptor 5, NMDA receptor 2B, GluR2, and GABAARα2 levels were not altered...
  86. Chiamulera C, Marzo C, Balfour D. Metabotropic glutamate receptor 5 as a potential target for smoking cessation. Psychopharmacology (Berl). 2017;234:1357-1370 pubmed publisher to review the evidence from preclinical and clinical studies that drugs that antagonise the metabotropic glutamate receptor 5 (mGluR5) in the brain are likely to be efficacious as treatments for tobacco dependence...
  87. Chiamulera C, Padovani L, Corsi M. Drug discovery for the treatment of substance use disorders: novel targets, repurposing, and the need for new paradigms. Curr Opin Pharmacol. 2017;35:120-124 pubmed publisher
    ..This review focus on known targets (e.g., metabotropic glutamate receptor 5 and GABAB receptor) and on novel potential treatment acting on oxytocin system, which interacts ..
  88. 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...
  89. de Dios Barajas López J, Moreno J, Gámez Arjona F, Pardo J, Punkkinen M, Zhu J, et al. Upstream kinases of plant SnRKs are involved in salt stress tolerance. Plant J. 2017;: pubmed publisher
    ..Rep-Interacting Kinase (GRIK)1 and GRIK2 phosphorylate SnRK1s, which are involved in sugar/energy sensing, and the grik1-1 grik2-1 double mutant shows growth retardation under regular growth conditions...
  90. Enz R. The actin-binding protein Filamin-A interacts with the metabotropic glutamate receptor type 7. FEBS Lett. 2002;514:184-8 pubmed
    ..Finally, co-expression of Filamin-A and mGluR7 splice variants was shown in brain regions. These findings suggest that Filamin-A may physically link metabotropic glutamate receptors to the actin cytoskeleton. ..
  91. Hirbec H, Francis J, Lauri S, Braithwaite S, Coussen F, Mulle C, et al. Rapid and differential regulation of AMPA and kainate receptors at hippocampal mossy fibre synapses by PICK1 and GRIP. Neuron. 2003;37:625-38 pubmed
    ..proteins, syntenin, PICK1, GRIP, and PSD95, as interactors with the kainate receptor (KAR) subunits GluR5(2b,) GluR5(2c), and GluR6...
  92. Wilding T, Zhou Y, Huettner J. Q/R site editing controls kainate receptor inhibition by membrane fatty acids. J Neurosci. 2005;25:9470-8 pubmed
    ..Genomic sequences for the glutamate receptor 2 (GluR2) subunit of AMPA receptors and the GluR5 and GluR6 subunits of kainate receptors all encode a neutral glutamine (Q) residue within the channel pore that ..