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Metabotropic glutamate receptor 1

January 01, 1970

The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 (mGluR1) protein.[5][6][7]

GRM1
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesGRM1, GPRC1A, MGLU1, MGLUR1, PPP1R85, SCAR13, glutamate metabotropic receptor 1, SCA44
External IDsOMIM: 604473 MGI: 1351338 HomoloGene: 649 GeneCards: GRM1
Orthologs
SpeciesHumanMouse
Entrez

2911

14816

Ensembl

ENSG00000152822

ENSMUSG00000019828

UniProt

Q13255

P97772

RefSeq (mRNA)

NM_001114333
NM_016976

RefSeq (protein)

NP_001264993
NP_001264994
NP_001264995
NP_001264996

NP_001107805
NP_058672

Location (UCSC)Chr 6: 146.03 – 146.44 MbChr 10: 10.56 – 10.96 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Function edit

L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions. The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group I, which includes GRM1 alongside GRM5, have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. Alternative splice variants of the GRM1 gene have been described but their full-length nature has not been determined.[5]

A possible connection has been suggested between mGluRs and neuromodulators, as mGluR1 antagonists block adrenergic receptor activation in neurons.[8]

Studies with knockout mice edit

Mice lacking functional glutamate receptor 1 were reported in 1994. By homologous recombination mediated gene targeting those mice became deficient in mGlu receptor 1 protein. The mice did not show any basic anatomical changes in the brain but had impaired cerebellar long-term depression and hippocampal long-term potentiation. In addition they had impaired motor functions, characterized by impaired balance. In the Morris watermaze test, an assay for learning abilities, those mice needed significantly more time to successfully complete the task.[9]

Clinical significance edit

Mutations in the GRM1 gene may contribute to melanoma susceptibility.[10] Antibodies against mGluR1 receptors cause cerebellar ataxia and impair long-term depression (LTDpathies) in the cerebellum.[11]

Ligands edit

In addition to the orthosteric site (the site where the endogenous ligand glutamate binds) at least two distinct allosteric binding sites exist on the mGluR1.[12] A respectable number of potent and specific allosteric ligands – predominantly antagonists/inhibitors – has been developed in recent years, although no orthosteric subtype-selective ligands have yet been discovered (2008).[13]

  • JNJ-16259685: highly potent, selective non-competitive antagonist[14]
  • R-214,127 and [3H]-analog: high-affinity, selective allosteric inhibitor[15]
  • YM-202,074: high-affinity, selective allosteric antagonist[16]
  • YM-230,888: high-affinity, selective allosteric antagonist[17]
  • YM-298,198 and [3H]-analog: selective non-competitive antagonist[18]
  • FTIDC: highly potent and selective allosteric antagonist/inverse agonist[19]
  • A-841,720: potent non-competitive antagonist; minor hmGluR5 binding[20]
  • VU-71: potentiator[12]
  • Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides: orally available PAMs[21]
  • Cyclothiazide: selective non-competitive antagonist of the mGluR1[22] (also AMPA potentiator and minor mGluR5 potentiator but not antagonist[23])
  • Riluzole : selective non-competitive antagonist[24]
  • Theanine : possible indirect inhibitor[25]
 
Chemical structures of mGluR1 selective ligands.

See also edit

References edit

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000152822 – Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000019828 – Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ a b "Entrez Gene: GRM1 glutamate receptor, metabotropic 1".
  6. ^ Stephan D, Bon C, Holzwarth JA, Galvan M, Pruss RM (1996). "Human metabotropic glutamate receptor 1: mRNA distribution, chromosome localization and functional expression of two splice variants". Neuropharmacology. 35 (12): 1649–1660. doi:10.1016/S0028-3908(96)00108-6. PMID 9076744. S2CID 37222391.
  7. ^ Makoff AJ, Phillips T, Pilling C, Emson P (September 1997). "Expression of a novel splice variant of human mGluR1 in the cerebellum". NeuroReport. 8 (13): 2943–2947. doi:10.1097/00001756-199709080-00027. PMID 9376535. S2CID 28116484.
  8. ^ Smith RS, Weitz CJ, Araneda RC (August 2009). "Excitatory actions of noradrenaline and metabotropic glutamate receptor activation in granule cells of the accessory olfactory bulb". Journal of Neurophysiology. 102 (2): 1103–1114. doi:10.1152/jn.91093.2008. PMC 2724365. PMID 19474170.
  9. ^ Conquet F, Bashir ZI, Davies CH, Daniel H, Ferraguti F, Bordi F, et al. (November 1994). "Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1". Nature. 372 (6503): 237–243. Bibcode:1994Natur.372..237C. doi:10.1038/372237a0. PMID 7969468. S2CID 4256888.
  10. ^ Ortiz P, Vanaclocha F, López-Bran E, Esquivias JI, López-Estebaranz JL, Martín-González M, et al. (November 2007). "Genetic analysis of the GRM1 gene in human melanoma susceptibility". European Journal of Human Genetics. 15 (11): 1176–1182. doi:10.1038/sj.ejhg.5201887. PMID 17609672.
  11. ^ Mitoma H, Honnorat J, Yamaguchi K, Manto M (December 2021). "LTDpathies: a Novel Clinical Concept". Cerebellum. 20 (6): 948–951. doi:10.1007/s12311-021-01259-2. PMC 8674158. PMID 33754326.
  12. ^ a b Hemstapat K, de Paulis T, Chen Y, Brady AE, Grover VK, Alagille D, et al. (August 2006). "A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators". Molecular Pharmacology. 70 (2): 616–626. doi:10.1124/mol.105.021857. PMID 16645124. S2CID 2719603.
  13. ^ based on a plain PubMed review
  14. ^ Lavreysen H, Wouters R, Bischoff F, Nóbrega Pereira S, Langlois X, Blokland S, et al. (December 2004). "JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist". Neuropharmacology. 47 (7): 961–972. doi:10.1016/j.neuropharm.2004.08.007. PMID 15555631. S2CID 601322.
  15. ^ Lavreysen H, Janssen C, Bischoff F, Langlois X, Leysen JE, Lesage AS (May 2003). "[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists". Molecular Pharmacology. 63 (5): 1082–1093. doi:10.1124/mol.63.5.1082. PMID 12695537.
  16. ^ Kohara A, Takahashi M, Yatsugi S, Tamura S, Shitaka Y, Hayashibe S, et al. (January 2008). "Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models". Brain Research. 1191: 168–179. doi:10.1016/j.brainres.2007.11.035. PMID 18164695. S2CID 3236484.
  17. ^ Kohara A, Nagakura Y, Kiso T, Toya T, Watabiki T, Tamura S, et al. (September 2007). "Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models". European Journal of Pharmacology. 571 (1): 8–16. doi:10.1016/j.ejphar.2007.05.030. PMID 17597604.
  18. ^ Kohara A, Toya T, Tamura S, Watabiki T, Nagakura Y, Shitaka Y, et al. (October 2005). "Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1". The Journal of Pharmacology and Experimental Therapeutics. 315 (1): 163–169. doi:10.1124/jpet.105.087171. PMID 15976016. S2CID 15291494.
  19. ^ Suzuki G, Kimura T, Satow A, Kaneko N, Fukuda J, Hikichi H, et al. (June 2007). "Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC)". The Journal of Pharmacology and Experimental Therapeutics. 321 (3): 1144–1153. doi:10.1124/jpet.106.116574. PMID 17360958. S2CID 10065500.
  20. ^ El-Kouhen O, Lehto SG, Pan JB, Chang R, Baker SJ, Zhong C, et al. (November 2006). "Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist". British Journal of Pharmacology. 149 (6): 761–774. doi:10.1038/sj.bjp.0706877. PMC 2014656. PMID 17016515.
  21. ^ Vieira E, Huwyler J, Jolidon S, Knoflach F, Mutel V, Wichmann J (March 2009). "Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers". Bioorganic & Medicinal Chemistry Letters. 19 (6): 1666–1669. doi:10.1016/j.bmcl.2009.01.108. PMID 19233648.
  22. ^ Surin A, Pshenichkin S, Grajkowska E, Surina E, Wroblewski JT (March 2007). "Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists". Neuropharmacology. 52 (3): 744–754. doi:10.1016/j.neuropharm.2006.09.018. PMC 1876747. PMID 17095021.
  23. ^ Surin A, Pshenichkin S, Grajkowska E, Surina E, Wroblewski JT (March 2007). "Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists". Neuropharmacology. 52 (3): 744–754. doi:10.1016/j.neuropharm.2006.09.018. PMC 1876747. PMID 17095021.
  24. ^ Lemieszek MK, Stepulak A, Sawa-Wejksza K, Czerwonka A, Ikonomidou C, Rzeski W (2018). "Riluzole Inhibits Proliferation, Migration and Cell Cycle Progression and Induces Apoptosis in Tumor Cells of Various Origins". Anti-Cancer Agents in Medicinal Chemistry. 18 (4): 565–572. doi:10.2174/1871520618666180228152713. PMID 29493465. S2CID 3605151.
  25. ^ Nagasawa K, Aoki H, Yasuda E, Nagai K, Shimohama S, Fujimoto S (July 2004). "Possible involvement of group I mGluRs in neuroprotective effect of theanine". Biochemical and Biophysical Research Communications. 320 (1): 116–122. doi:10.1016/j.bbrc.2004.05.143. PMID 15207710.

Further reading edit

  • Bockaert J, Pin JP (April 1999). "Molecular tinkering of G protein-coupled receptors: an evolutionary success". The EMBO Journal. 18 (7): 1723–1729. doi:10.1093/emboj/18.7.1723. PMC 1171258. PMID 10202136.
  • King JE, Eugenin EA, Buckner CM, Berman JW (April 2006). "HIV tat and neurotoxicity". Microbes and Infection. 8 (5): 1347–1357. doi:10.1016/j.micinf.2005.11.014. PMID 16697675.
  • Desai MA, Burnett JP, Mayne NG, Schoepp DD (October 1995). "Cloning and expression of a human metabotropic glutamate receptor 1 alpha: enhanced coupling on co-transfection with a glutamate transporter". Molecular Pharmacology. 48 (4): 648–657. PMID 7476890.
  • Scherer SW, Duvoisin RM, Kuhn R, Heng HH, Belloni E, Tsui LC (January 1996). "Localization of two metabotropic glutamate receptor genes, GRM3 and GRM8, to human chromosome 7q". Genomics. 31 (2): 230–233. doi:10.1006/geno.1996.0036. PMID 8824806.
  • Brakeman PR, Lanahan AA, O'Brien R, Roche K, Barnes CA, Huganir RL, Worley PF (March 1997). "Homer: a protein that selectively binds metabotropic glutamate receptors". Nature. 386 (6622): 284–288. Bibcode:1997Natur.386..284B. doi:10.1038/386284a0. PMID 9069287. S2CID 4346579.
  • Stephan D, Bon C, Holzwarth JA, Galvan M, Pruss RM (1997). "Human metabotropic glutamate receptor 1: mRNA distribution, chromosome localization and functional expression of two splice variants". Neuropharmacology. 35 (12): 1649–1660. doi:10.1016/S0028-3908(96)00108-6. PMID 9076744. S2CID 37222391.
  • Makoff AJ, Phillips T, Pilling C, Emson P (September 1997). "Expression of a novel splice variant of human mGluR1 in the cerebellum". NeuroReport. 8 (13): 2943–2947. doi:10.1097/00001756-199709080-00027. PMID 9376535. S2CID 28116484.
  • Francesconi A, Duvoisin RM (March 1998). "Role of the second and third intracellular loops of metabotropic glutamate receptors in mediating dual signal transduction activation". The Journal of Biological Chemistry. 273 (10): 5615–5624. doi:10.1074/jbc.273.10.5615. PMID 9488690.
  • Okamoto T, Sekiyama N, Otsu M, Shimada Y, Sato A, Nakanishi S, Jingami H (May 1998). "Expression and purification of the extracellular ligand binding region of metabotropic glutamate receptor subtype 1". The Journal of Biological Chemistry. 273 (21): 13089–13096. doi:10.1074/jbc.273.21.13089. PMID 9582347.
  • Snow BE, Hall RA, Krumins AM, Brothers GM, Bouchard D, Brothers CA, et al. (July 1998). "GTPase activating specificity of RGS12 and binding specificity of an alternatively spliced PDZ (PSD-95/Dlg/ZO-1) domain". The Journal of Biological Chemistry. 273 (28): 17749–17755. doi:10.1074/jbc.273.28.17749. PMID 9651375.
  • Xiao B, Tu JC, Petralia RS, Yuan JP, Doan A, Breder CD, et al. (October 1998). "Homer regulates the association of group 1 metabotropic glutamate receptors with multivalent complexes of homer-related, synaptic proteins". Neuron. 21 (4): 707–716. doi:10.1016/S0896-6273(00)80588-7. PMID 9808458. S2CID 16431031.
  • Tu JC, Xiao B, Yuan JP, Lanahan AA, Leoffert K, Li M, et al. (October 1998). "Homer binds a novel proline-rich motif and links group 1 metabotropic glutamate receptors with IP3 receptors". Neuron. 21 (4): 717–726. doi:10.1016/S0896-6273(00)80589-9. PMID 9808459. S2CID 2851554.
  • Ciruela F, Robbins MJ, Willis AC, McIlhinney RA (January 1999). "Interactions of the C terminus of metabotropic glutamate receptor type 1alpha with rat brain proteins: evidence for a direct interaction with tubulin". Journal of Neurochemistry. 72 (1): 346–354. doi:10.1046/j.1471-4159.1999.0720346.x. PMID 9886087. S2CID 3923065.
  • Robbins MJ, Ciruela F, Rhodes A, McIlhinney RA (June 1999). "Characterization of the dimerization of metabotropic glutamate receptors using an N-terminal truncation of mGluR1alpha". Journal of Neurochemistry. 72 (6): 2539–2547. doi:10.1046/j.1471-4159.1999.0722539.x. PMID 10349865. S2CID 43073802.
  • Mody N, Hermans E, Nahorski SR, Challiss RA (October 1999). "Inhibition of N-linked glycosylation of the human type 1alpha metabotropic glutamate receptor by tunicamycin: effects on cell-surface receptor expression and function". Neuropharmacology. 38 (10): 1485–1492. doi:10.1016/S0028-3908(99)00099-4. PMID 10530810. S2CID 31175440.
  • Francesconi A, Duvoisin RM (May 2000). "Opposing effects of protein kinase C and protein kinase A on metabotropic glutamate receptor signaling: selective desensitization of the inositol trisphosphate/Ca2+ pathway by phosphorylation of the receptor-G protein-coupling domain". Proceedings of the National Academy of Sciences of the United States of America. 97 (11): 6185–6190. Bibcode:2000PNAS...97.6185F. doi:10.1073/pnas.97.11.6185. PMC 18579. PMID 10823959.
  • Ganesh S, Amano K, Yamakawa K (2000). "Assignment of the gene GRM1 coding for metabotropic glutamate receptor 1 to human chromosome band 6q24 by in situ hybridization". Cytogenetics and Cell Genetics. 88 (3–4): 314–315. doi:10.1159/000015517. PMID 10828618. S2CID 26499807.
  • Ray K, Hauschild BC (November 2000). "Cys-140 is critical for metabotropic glutamate receptor-1 dimerization". The Journal of Biological Chemistry. 275 (44): 34245–34251. doi:10.1074/jbc.M005581200. PMID 10945991.
  • Hartley JL, Temple GF, Brasch MA (November 2000). "DNA cloning using in vitro site-specific recombination". Genome Research. 10 (11): 1788–1795. doi:10.1101/gr.143000. PMC 310948. PMID 11076863.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


External links edit

  • . IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2008-12-05.
  • Overview of all the structural information available in the PDB for UniProt: Q13255 (Metabotropic glutamate receptor 1) at the PDBe-KB.

January 01, 1970
metabotropic, glutamate, receptor, glutamate, receptor, metabotropic, also, known, grm1, human, gene, which, encodes, metabotropic, glutamate, receptor, mglur1, protein, grm1available, structurespdbortholog, search, pdbe, rcsblist, codes3ks9, 4or2identifiersal. The glutamate receptor metabotropic 1 also known as GRM1 is a human gene which encodes the metabotropic glutamate receptor 1 mGluR1 protein 5 6 7 GRM1Available structuresPDBOrtholog search PDBe RCSBList of PDB id codes3KS9 4OR2IdentifiersAliasesGRM1 GPRC1A MGLU1 MGLUR1 PPP1R85 SCAR13 glutamate metabotropic receptor 1 SCA44External IDsOMIM 604473 MGI 1351338 HomoloGene 649 GeneCards GRM1Gene location Human Chr Chromosome 6 human 1 Band6q24 3Start146 027 646 bp 1 End146 437 601 bp 1 Gene location Mouse Chr Chromosome 10 mouse 2 Band10 10 A1Start10 561 803 bp 2 End10 958 100 bp 2 RNA expression patternBgeeHumanMouse ortholog Top expressed incerebellar vermismiddle temporal gyrusendothelial cellBrodmann area 23cerebellar hemisphereponsoptic nervesuperior frontal gyrusBrodmann area 46postcentral gyrusTop expressed inmedial dorsal nucleusmedial geniculate nucleuslateral geniculate nucleuscerebellar vermismammillary bodysuperior colliculusglobus palliduslateral hypothalamusolfactory tubercledorsomedial hypothalamic nucleusMore reference expression dataBioGPSMore reference expression dataGene ontologyMolecular functionglutamate receptor activity G protein coupled receptor activity signal transducer activity protein binding neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration identical protein binding G protein coupled neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration G protein coupled receptor activity involved in regulation of postsynaptic membrane potentialCellular componentintegral component of membrane G protein coupled receptor dimeric complex postsynaptic density membrane G protein coupled receptor homodimeric complex plasma membrane integral component of plasma membrane dendrite neuron projection nucleus presynaptic membrane Schaffer collateral CA1 synapse glutamatergic synapse postsynaptic density membraneBiological processcellular response to electrical stimulus G protein coupled glutamate receptor signaling pathway positive regulation of cytosolic calcium ion concentration involved in phospholipase C activating G protein coupled signaling pathway regulation of MAPK cascade regulation of sensory perception of pain locomotory behavior sensory perception of pain signal transduction chemical synaptic transmission regulation of synaptic transmission glutamatergic adenylate cyclase inhibiting G protein coupled glutamate receptor signaling pathway regulation of postsynaptic cytosolic calcium ion concentration G protein coupled receptor signaling pathway regulation of postsynaptic membrane potentialSources Amigo QuickGOOrthologsSpeciesHumanMouseEntrez291114816EnsemblENSG00000152822ENSMUSG00000019828UniProtQ13255P97772RefSeq mRNA NM 000838NM 001114329NM 001278064NM 001278065NM 001278066NM 001278067NM 001114333NM 016976RefSeq protein NP 001264993NP 001264994NP 001264995NP 001264996NP 001107805NP 058672Location UCSC Chr 6 146 03 146 44 MbChr 10 10 56 10 96 MbPubMed search 3 4 WikidataView Edit HumanView Edit Mouse Contents 1 Function 2 Studies with knockout mice 3 Clinical significance 4 Ligands 5 See also 6 References 7 Further reading 8 External linksFunction editL glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions The metabotropic glutamate receptors are a family of G protein coupled receptors that have been divided into 3 groups on the basis of sequence homology putative signal transduction mechanisms and pharmacologic properties Group I which includes GRM1 alongside GRM5 have been shown to activate phospholipase C Group II includes GRM2 and GRM3 while Group III includes GRM4 GRM6 GRM7 and GRM8 Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities Alternative splice variants of the GRM1 gene have been described but their full length nature has not been determined 5 A possible connection has been suggested between mGluRs and neuromodulators as mGluR1 antagonists block adrenergic receptor activation in neurons 8 Studies with knockout mice editMice lacking functional glutamate receptor 1 were reported in 1994 By homologous recombination mediated gene targeting those mice became deficient in mGlu receptor 1 protein The mice did not show any basic anatomical changes in the brain but had impaired cerebellar long term depression and hippocampal long term potentiation In addition they had impaired motor functions characterized by impaired balance In the Morris watermaze test an assay for learning abilities those mice needed significantly more time to successfully complete the task 9 Clinical significance editMutations in the GRM1 gene may contribute to melanoma susceptibility 10 Antibodies against mGluR1 receptors cause cerebellar ataxia and impair long term depression LTDpathies in the cerebellum 11 Ligands editIn addition to the orthosteric site the site where the endogenous ligand glutamate binds at least two distinct allosteric binding sites exist on the mGluR1 12 A respectable number of potent and specific allosteric ligands predominantly antagonists inhibitors has been developed in recent years although no orthosteric subtype selective ligands have yet been discovered 2008 13 JNJ 16259685 highly potent selective non competitive antagonist 14 R 214 127 and 3H analog high affinity selective allosteric inhibitor 15 YM 202 074 high affinity selective allosteric antagonist 16 YM 230 888 high affinity selective allosteric antagonist 17 YM 298 198 and 3H analog selective non competitive antagonist 18 FTIDC highly potent and selective allosteric antagonist inverse agonist 19 A 841 720 potent non competitive antagonist minor hmGluR5 binding 20 VU 71 potentiator 12 Fluorinated 9H xanthene 9 carboxylic acid oxazol 2 yl amides orally available PAMs 21 Cyclothiazide selective non competitive antagonist of the mGluR1 22 also AMPA potentiator and minor mGluR5 potentiator but not antagonist 23 Riluzole selective non competitive antagonist 24 Theanine possible indirect inhibitor 25 nbsp Chemical structures of mGluR1 selective ligands See also editMetabotropic glutamate receptorReferences edit a b c GRCh38 Ensembl release 89 ENSG00000152822 Ensembl May 2017 a b c GRCm38 Ensembl release 89 ENSMUSG00000019828 Ensembl May 2017 Human PubMed Reference National Center for Biotechnology Information U S National Library of Medicine Mouse PubMed Reference National Center for Biotechnology Information U S National Library of Medicine a b Entrez Gene GRM1 glutamate receptor metabotropic 1 Stephan D Bon C Holzwarth JA Galvan M Pruss RM 1996 Human metabotropic glutamate receptor 1 mRNA distribution chromosome localization and functional expression of two splice variants Neuropharmacology 35 12 1649 1660 doi 10 1016 S0028 3908 96 00108 6 PMID 9076744 S2CID 37222391 Makoff AJ Phillips T Pilling C Emson P September 1997 Expression of a novel splice variant of human mGluR1 in the cerebellum NeuroReport 8 13 2943 2947 doi 10 1097 00001756 199709080 00027 PMID 9376535 S2CID 28116484 Smith RS Weitz CJ Araneda RC August 2009 Excitatory actions of noradrenaline and metabotropic glutamate receptor activation in granule cells of the accessory olfactory bulb Journal of Neurophysiology 102 2 1103 1114 doi 10 1152 jn 91093 2008 PMC 2724365 PMID 19474170 Conquet F Bashir ZI Davies CH Daniel H Ferraguti F Bordi F et al November 1994 Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1 Nature 372 6503 237 243 Bibcode 1994Natur 372 237C doi 10 1038 372237a0 PMID 7969468 S2CID 4256888 Ortiz P Vanaclocha F Lopez Bran E Esquivias JI Lopez Estebaranz JL Martin Gonzalez M et al November 2007 Genetic analysis of the GRM1 gene in human melanoma susceptibility European Journal of Human Genetics 15 11 1176 1182 doi 10 1038 sj ejhg 5201887 PMID 17609672 Mitoma H Honnorat J Yamaguchi K Manto M December 2021 LTDpathies a Novel Clinical Concept Cerebellum 20 6 948 951 doi 10 1007 s12311 021 01259 2 PMC 8674158 PMID 33754326 a b Hemstapat K de Paulis T Chen Y Brady AE Grover VK Alagille D et al August 2006 A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators Molecular Pharmacology 70 2 616 626 doi 10 1124 mol 105 021857 PMID 16645124 S2CID 2719603 based on a plain PubMed review Lavreysen H Wouters R Bischoff F Nobrega Pereira S Langlois X Blokland S et al December 2004 JNJ16259685 a highly potent selective and systemically active mGlu1 receptor antagonist Neuropharmacology 47 7 961 972 doi 10 1016 j neuropharm 2004 08 007 PMID 15555631 S2CID 601322 Lavreysen H Janssen C Bischoff F Langlois X Leysen JE Lesage AS May 2003 3H R214127 a novel high affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists Molecular Pharmacology 63 5 1082 1093 doi 10 1124 mol 63 5 1082 PMID 12695537 Kohara A Takahashi M Yatsugi S Tamura S Shitaka Y Hayashibe S et al January 2008 Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM 202074 in rat stroke models Brain Research 1191 168 179 doi 10 1016 j brainres 2007 11 035 PMID 18164695 S2CID 3236484 Kohara A Nagakura Y Kiso T Toya T Watabiki T Tamura S et al September 2007 Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM 230888 in chronic pain rodent models European Journal of Pharmacology 571 1 8 16 doi 10 1016 j ejphar 2007 05 030 PMID 17597604 Kohara A Toya T Tamura S Watabiki T Nagakura Y Shitaka Y et al October 2005 Radioligand binding properties and pharmacological characterization of 6 amino N cyclohexyl N 3 dimethylthiazolo 3 2 a benzimidazole 2 carboxamide YM 298198 a high affinity selective and noncompetitive antagonist of metabotropic glutamate receptor type 1 The Journal of Pharmacology and Experimental Therapeutics 315 1 163 169 doi 10 1124 jpet 105 087171 PMID 15976016 S2CID 15291494 Suzuki G Kimura T Satow A Kaneko N Fukuda J Hikichi H et al June 2007 Pharmacological characterization of a new orally active and potent allosteric metabotropic glutamate receptor 1 antagonist 4 1 2 fluoropyridin 3 yl 5 methyl 1H 1 2 3 triazol 4 yl N isopropyl N methyl 3 6 dihydropyridine 1 2H carboxamide FTIDC The Journal of Pharmacology and Experimental Therapeutics 321 3 1144 1153 doi 10 1124 jpet 106 116574 PMID 17360958 S2CID 10065500 El Kouhen O Lehto SG Pan JB Chang R Baker SJ Zhong C et al November 2006 Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances effects of A 841720 a novel non competitive mGluR1 receptor antagonist British Journal of Pharmacology 149 6 761 774 doi 10 1038 sj bjp 0706877 PMC 2014656 PMID 17016515 Vieira E Huwyler J Jolidon S Knoflach F Mutel V Wichmann J March 2009 Fluorinated 9H xanthene 9 carboxylic acid oxazol 2 yl amides as potent orally available mGlu1 receptor enhancers Bioorganic amp Medicinal Chemistry Letters 19 6 1666 1669 doi 10 1016 j bmcl 2009 01 108 PMID 19233648 Surin A Pshenichkin S Grajkowska E Surina E Wroblewski JT March 2007 Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non competitive antagonists Neuropharmacology 52 3 744 754 doi 10 1016 j neuropharm 2006 09 018 PMC 1876747 PMID 17095021 Surin A Pshenichkin S Grajkowska E Surina E Wroblewski JT March 2007 Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non competitive antagonists Neuropharmacology 52 3 744 754 doi 10 1016 j neuropharm 2006 09 018 PMC 1876747 PMID 17095021 Lemieszek MK Stepulak A Sawa Wejksza K Czerwonka A Ikonomidou C Rzeski W 2018 Riluzole Inhibits Proliferation Migration and Cell Cycle Progression and Induces Apoptosis in Tumor Cells of Various Origins Anti Cancer Agents in Medicinal Chemistry 18 4 565 572 doi 10 2174 1871520618666180228152713 PMID 29493465 S2CID 3605151 Nagasawa K Aoki H Yasuda E Nagai K Shimohama S Fujimoto S July 2004 Possible involvement of group I mGluRs in neuroprotective effect of theanine Biochemical and Biophysical Research Communications 320 1 116 122 doi 10 1016 j bbrc 2004 05 143 PMID 15207710 Further reading editBockaert J Pin JP April 1999 Molecular tinkering of G protein coupled receptors an evolutionary success The EMBO Journal 18 7 1723 1729 doi 10 1093 emboj 18 7 1723 PMC 1171258 PMID 10202136 King JE Eugenin EA Buckner CM Berman JW April 2006 HIV tat and neurotoxicity Microbes and Infection 8 5 1347 1357 doi 10 1016 j micinf 2005 11 014 PMID 16697675 Desai MA Burnett JP Mayne NG Schoepp DD October 1995 Cloning and expression of a human metabotropic glutamate receptor 1 alpha enhanced coupling on co transfection with a glutamate transporter Molecular Pharmacology 48 4 648 657 PMID 7476890 Scherer SW Duvoisin RM Kuhn R Heng HH Belloni E Tsui LC January 1996 Localization of two metabotropic glutamate receptor genes GRM3 and GRM8 to human chromosome 7q Genomics 31 2 230 233 doi 10 1006 geno 1996 0036 PMID 8824806 Brakeman PR Lanahan AA O Brien R Roche K Barnes CA Huganir RL Worley PF March 1997 Homer a protein that selectively binds metabotropic glutamate receptors Nature 386 6622 284 288 Bibcode 1997Natur 386 284B doi 10 1038 386284a0 PMID 9069287 S2CID 4346579 Stephan D Bon C Holzwarth JA Galvan M Pruss RM 1997 Human metabotropic glutamate receptor 1 mRNA distribution chromosome localization and functional expression of two splice variants Neuropharmacology 35 12 1649 1660 doi 10 1016 S0028 3908 96 00108 6 PMID 9076744 S2CID 37222391 Makoff AJ Phillips T Pilling C Emson P September 1997 Expression of a novel splice variant of human mGluR1 in the cerebellum NeuroReport 8 13 2943 2947 doi 10 1097 00001756 199709080 00027 PMID 9376535 S2CID 28116484 Francesconi A Duvoisin RM March 1998 Role of the second and third intracellular loops of metabotropic glutamate receptors in mediating dual signal transduction activation The Journal of Biological Chemistry 273 10 5615 5624 doi 10 1074 jbc 273 10 5615 PMID 9488690 Okamoto T Sekiyama N Otsu M Shimada Y Sato A Nakanishi S Jingami H May 1998 Expression and purification of the extracellular ligand binding region of metabotropic glutamate receptor subtype 1 The Journal of Biological Chemistry 273 21 13089 13096 doi 10 1074 jbc 273 21 13089 PMID 9582347 Snow BE Hall RA Krumins AM Brothers GM Bouchard D Brothers CA et al July 1998 GTPase activating specificity of RGS12 and binding specificity of an alternatively spliced PDZ PSD 95 Dlg ZO 1 domain The Journal of Biological Chemistry 273 28 17749 17755 doi 10 1074 jbc 273 28 17749 PMID 9651375 Xiao B Tu JC Petralia RS Yuan JP Doan A Breder CD et al October 1998 Homer regulates the association of group 1 metabotropic glutamate receptors with multivalent complexes of homer related synaptic proteins Neuron 21 4 707 716 doi 10 1016 S0896 6273 00 80588 7 PMID 9808458 S2CID 16431031 Tu JC Xiao B Yuan JP Lanahan AA Leoffert K Li M et al October 1998 Homer binds a novel proline rich motif and links group 1 metabotropic glutamate receptors with IP3 receptors Neuron 21 4 717 726 doi 10 1016 S0896 6273 00 80589 9 PMID 9808459 S2CID 2851554 Ciruela F Robbins MJ Willis AC McIlhinney RA January 1999 Interactions of the C terminus of metabotropic glutamate receptor type 1alpha with rat brain proteins evidence for a direct interaction with tubulin Journal of Neurochemistry 72 1 346 354 doi 10 1046 j 1471 4159 1999 0720346 x PMID 9886087 S2CID 3923065 Robbins MJ Ciruela F Rhodes A McIlhinney RA June 1999 Characterization of the dimerization of metabotropic glutamate receptors using an N terminal truncation of mGluR1alpha Journal of Neurochemistry 72 6 2539 2547 doi 10 1046 j 1471 4159 1999 0722539 x PMID 10349865 S2CID 43073802 Mody N Hermans E Nahorski SR Challiss RA October 1999 Inhibition of N linked glycosylation of the human type 1alpha metabotropic glutamate receptor by tunicamycin effects on cell surface receptor expression and function Neuropharmacology 38 10 1485 1492 doi 10 1016 S0028 3908 99 00099 4 PMID 10530810 S2CID 31175440 Francesconi A Duvoisin RM May 2000 Opposing effects of protein kinase C and protein kinase A on metabotropic glutamate receptor signaling selective desensitization of the inositol trisphosphate Ca2 pathway by phosphorylation of the receptor G protein coupling domain Proceedings of the National Academy of Sciences of the United States of America 97 11 6185 6190 Bibcode 2000PNAS 97 6185F doi 10 1073 pnas 97 11 6185 PMC 18579 PMID 10823959 Ganesh S Amano K Yamakawa K 2000 Assignment of the gene GRM1 coding for metabotropic glutamate receptor 1 to human chromosome band 6q24 by in situ hybridization Cytogenetics and Cell Genetics 88 3 4 314 315 doi 10 1159 000015517 PMID 10828618 S2CID 26499807 Ray K Hauschild BC November 2000 Cys 140 is critical for metabotropic glutamate receptor 1 dimerization The Journal of Biological Chemistry 275 44 34245 34251 doi 10 1074 jbc M005581200 PMID 10945991 Hartley JL Temple GF Brasch MA November 2000 DNA cloning using in vitro site specific recombination Genome Research 10 11 1788 1795 doi 10 1101 gr 143000 PMC 310948 PMID 11076863 This article incorporates text from the United States National Library of Medicine which is in the public domain External links edit Metabotropic Glutamate Receptors mGlu1 IUPHAR Database of Receptors and Ion Channels International Union of Basic and Clinical Pharmacology Archived from the original on 2016 03 03 Retrieved 2008 12 05 Overview of all the structural information available in the PDB for UniProt Q13255 Metabotropic glutamate receptor 1 at the PDBe KB Retrieved from https en wikipedia org w 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