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mGlu3 receptor

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Target not currently curated in GtoImmuPdb

Target id: 291

Nomenclature: mGlu3 receptor

Family: Metabotropic glutamate receptors

Contents:

Gene and Protein Information Click here for help
class C G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 879 7q21.11-q21.12 GRM3 glutamate metabotropic receptor 3 6,18,26
Mouse 7 879 5 A1 Grm3 glutamate receptor, metabotropic 3 12
Rat 7 879 4q12 Grm3 glutamate metabotropic receptor 3 30
Previous and Unofficial Names Click here for help
mGluR3 | GPRC1C | glutamate receptor
Database Links Click here for help
Specialist databases
GPCRdb grm3_human (Hs), grm3_mouse (Mm), grm3_rat (Rn)
Other databases
Alphafold Q14832 (Hs), Q9QYS2 (Mm), P31422 (Rn)
ChEMBL Target CHEMBL2888 (Hs), CHEMBL3824 (Mm), CHEMBL3067 (Rn)
Ensembl Gene ENSG00000198822 (Hs), ENSMUSG00000003974 (Mm), ENSRNOG00000005519 (Rn)
Entrez Gene 2913 (Hs), 108069 (Mm), 24416 (Rn)
Human Protein Atlas ENSG00000198822 (Hs)
KEGG Gene hsa:2913 (Hs), mmu:108069 (Mm), rno:24416 (Rn)
OMIM 60115 (Hs)
Pharos Q14832 (Hs)
RefSeq Nucleotide NM_000840 (Hs), NM_181850 (Mm), NM_001105712 (Rn)
RefSeq Protein NP_000831 (Hs), NP_862898 (Mm), NP_001099182 (Rn)
UniProtKB Q14832 (Hs), Q9QYS2 (Mm), P31422 (Rn)
Wikipedia GRM3 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Metabotropic glutamate receptor 3 precursor in presence of LY341495 antagonist.
PDB Id:  3SM9
Ligand:  LY341495
Resolution:  2.26Å
Species:  Human
References:  33
Natural/Endogenous Ligands Click here for help
L-glutamic acid
NAAG
Comments: Other endogenous ligands include L-aspartic acid, L-serine-O-phosphate, NAAG and L-cysteine sulphinic acid

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LY341495 Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Full agonist 7.3 pKd 27
⤷ pKd 7.3 [27]
eglumegad Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.9 pKi 9
⤷ pKi 8.9 [9]
L-CCG-I Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 9
⤷ pKi 7.4 [9]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.4 pKi 9
⤷ pKi 7.4 [9]
eglumegad Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.3 pKi 27
⤷ pKi 7.3 [27]
DCG-IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.2 pKi 9
⤷ pKi 7.2 [9]
DCG-IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.8 pKi 27
⤷ pKi 6.8 [27]
L-CCG-I Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.5 pKi 27
⤷ pKi 6.5 [27]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.4 pKi 27
⤷ pKi 6.4 [27]
(2R,3R)-APDC Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.3 pKi 9
⤷ pKi 5.3 [9]
(1S,3R)-ACPD Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 4.8 pKi 27
⤷ pKi 4.8 [27]
LY379268 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.8 pKi 17
⤷ pKi 4.8 [17]
(1S,3R)-ACPD Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 4.7 pKi 9
⤷ pKi 4.7 [9]
NAAG Small molecule or natural product Ligand is endogenous in the given species Hs Full agonist 4.7 pKi 27
⤷ pKi 4.7 [27]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 5.3 – 5.4 pEC50 23
⤷ pEC50 5.3 – 5.4 [23]
View species-specific agonist tables
Agonist Comments
Affinities listed are from displacement of antagonist ([3H]LY341495) or agonist ([3H]LY354740) for the low and high values listed, respectively, in homogenates from mGlu3-expressing recombinant cell lines. Potency in functional assays can be found in the review article [26]. To date, no ligands have shown a difference in their affinity for rat or human mGlu3 receptors. Several of the above agonists are Group II mGlu (mGlu2/3) receptor selective verses the Group I and III receptors, with the exceptions of glutamate, and (1S,3R)-ACPD. The agonist binding site for mGlu3 has been studied by homology modeling and mutagenesis [16,35].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LY341495 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 9.1 pKd 9
⤷ pKd 9.1 [9]
LY341495 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.9 pKi 9
⤷ pKi 8.9 [9]
MGS0039 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.3 – 8.4 pKi 4,19
⤷ pKi 8.3 – 8.4 [4,19]
LY341495 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.0 pKi 27
⤷ pKi 8.0 [27]
LY395756 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 13
⤷ pKi 6.5 (Ki 3.02x10-7 M) [13]
eGlu Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.4 pKi 27
⤷ pKi 5.4 [27]
(+)-MCPG Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 3.8 pKi 9
⤷ pKi 3.8 [9]
View species-specific antagonist tables
Antagonist Comments
Affinities listed are from displacement of antagonist ([3H]LY341495) and/or agonist ([3H]LY354740) in homogenates of mGlu3-expressing recombinant cell lines. Potency in functional assays can be found in the review article 7. To date, no ligands have shown a difference in their affinity for rat or human mGlu3 receptors.
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
MNI-135 Small molecule or natural product Click here for species-specific activity table Rn Negative 7.5 pEC50 8
⤷ pEC50 7.5 (EC50 3.02x10-8 M) [8]
compound 3 [PMID: 21105727] Small molecule or natural product Click here for species-specific activity table Hs Positive 5.1 pEC50 25
⤷ pEC50 5.1 (EC50 8.9x10-6 M) [25]
compound 4 [PMID: 21105727] Small molecule or natural product Click here for species-specific activity table Hs Positive 5.0 pEC50 25
⤷ pEC50 5.0 (EC50 1.04x10-5 M) [25]
compound 2 [PMID: 21105727] Small molecule or natural product Click here for species-specific activity table Hs Positive 4.9 pEC50 25
⤷ pEC50 4.9 (EC50 1.34x10-5 M) [25]
Ro4491533 Small molecule or natural product Click here for species-specific activity table Rn Negative >8.0 pIC50 34
⤷ pIC50 >8.0 (IC50 <1x10-8 M) [34]
MNI-136 Small molecule or natural product Click here for species-specific activity table Rn Negative 7.7 pIC50 8
⤷ pIC50 7.7 (IC50 2.13x10-8 M) [8]
MNI-137 Small molecule or natural product Click here for species-specific activity table Rn Negative 7.7 pIC50 8
⤷ pIC50 7.7 (IC50 2.03x10-8 M) [8]
LY2389575 Small molecule or natural product Primary target of this compound Hs Negative 6.7 pIC50 28
⤷ pIC50 6.7 (IC50 1.9x10-7 M) [28]
Description: Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.
Ro4491533 Small molecule or natural product Click here for species-specific activity table Hs Negative 6.6 pIC50 3
⤷ pIC50 6.6 (IC50 2.7x10-7 M) [3]
VU0650786 Small molecule or natural product Hs Negative 6.4 pIC50 7
⤷ pIC50 6.4 [7]
ML337 Small molecule or natural product Primary target of this compound Rn Negative 6.2 pIC50 32
⤷ pIC50 6.2 (IC50 5.93x10-7 M) [32]
VU0463597 Small molecule or natural product Rn Negative 5.8 – 6.2 pIC50 28
⤷ pIC50 5.8 – 6.2 (IC50 1.5x10-6 – 6.6x10-7 M) [28]
View species-specific allosteric modulator tables
Allosteric Modulator Comments
Targeting the allosteric site of the mGlu3 receptor is being pursued for the development of selective compounds, especially vs. mGlu2, as orthosteric ligands have so far failed to provide sufficient selectivity. Of particular interest is the development of mGlu3 selective PAMs as potential leads for neurodegenerative diseases, and NAMs which are suggested to offer potential for the treatment of schizophrenia, depression or chronic pain.
MNI-135, MNI-136, and MNI-137 [8], and Compounds 2, 3 and 4 are also mGlu2 NAMs [25]. ML289 (VU0463597) is >10 µM potency vs. rat mGlu2.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
Potassium channel
Calcium channel
Comments:  Protein Kinase A, and L-type calcium channels
References:  36
Tissue Distribution Click here for help
In the human brain mGlu3 receptors are mainly localised in neurones.
Cerebellum (on the edge of the Purkinje cell layer, probably stellate cells, Golgi cells in the granule cell layer), cerebral cortex (particularly the deep layers IV-VI), hippocampus (granule cells of the dentate gyrus, caudate-putamen, reticular area of the thalamus).
Species:  Human
Technique:  Northern blotting.
References:  15
Within the brain, the mGlu3 receptor is localized both pre- and postsynaptically. It is also often found in glia and astrocytes.
Cerebral cortex, hippocampus (dentate gyrus > strata radiatum > stratum lucidum), olfactory system (anterior olfactory nucleus, olfactory tubercle, piriform cortex, nucleus of the lateral olfactory tract), basal ganglia and other subcortical regions in the forebrain (striatum and nucleus accumbens, globus pallidus > substantia nigra pars reticulata > ventral pallidum), thalamus and epithalamus, brainstem and spinal cord, cerebellum.
Species:  Mouse
Technique:  immunocytochemistry.
References:  29
Aanterior olfactory nucleus, cerebral neo- and mesocortical regions, lateral amygdaloid nucleus, ventral part of the basolateral amygdaloid nucleus, dorsal endopiriform nucleus, supraoptic nucleus, superficial layers of the superior colliculus, inferior colliculus, interpeduncular nucleus, superior olivary nuclei, and Golgi cells in the cerebellar cortex > striatum, nucleus accumbens, ventral pallidum, globus pallidus, entopeduncular nucleus, lateral hypothalamic area, hypothalamic paraventricular nucleus, medial habenular nucleus, anterior pretectal nucleus, Barrington's nucleus, Nucleus O, paragenual nucleus, trigeminal sensory complex, cochlear nuclei, dorsal motor nucleus of the trigeminal nerve, dorsal cap of the inferior olive, spinal dorsal horn, and lamina X of the spinal cord, stellate cells in the cerebellar cortex, neurons in the deep cerebellar nuclei.
Species:  Rat
Technique:  in situ hybridization.
References:  20
Islets of Langerhans and pancreatic alpha-cell and beta-cell lines.
Species:  Rat
Technique:  RT-PCR and immunoblot.
References:  2
Dorsal cochlear nucleus.
Species:  Rat
Technique:  immunocytochemistry.
References:  22
Reticular nucleus of the thalamus, rostral olfactory structures, hippocampus.
Species:  Rat
Technique:  immunocytochemistry.
References:  21
Reticular thalamic nucleus >> mediodorsal thalamic nucleus, centromedial/centrolateral thalamic nuclei, ventromedial thalamic nucleus > other thalamic nuclei.
Species:  Rat
Technique:  in situ hybridisation.
References:  14
Cerebral cortex and caudate putamen, granule cells of hippocampal dentate gyrus.
Species:  Rat
Technique:  in situ hybridization.
References:  31
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Native mGlu3 receptor function has been linked to the regulation of GABA release from the rat cortical neurons in primary culture.
Species:  Rat
Tissue:  Primary culture of cortical neurons.
Response measured:  [3H]-GABA release.
References:  36
mGlu3 receptor-mediated release of Nerve Growth factor from cultured astrocytes.
Species:  Rat
Tissue:  Secondary Glial cultures from primary rat cortical astrocytes.
Response measured:  Nerve Growth Factor release.
References:  5
Measurement of cAMP levels in CHO cells transfected with the rat mGlu3 receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP production.
References:  31
Measurement of cAMP levels in rat glutamate transporter (RGT) cells transfected with the mGlu3 receptor.
Species:  Human
Tissue:  RGT cells.
Response measured:  Inhibition of cAMP accumulation.
References:  11
Measurement of IP levels in HEK 293 cells transfected with the rat mGlu3 receptor and Gqi9.
Species:  Rat
Tissue:  HEK 293 cells.
Response measured:  IP accumulation.
References:  1
Physiological Functions Click here for help
MGlu3 activation is thought to inhibit synaptic transmission.
Species:  Rat
Tissue:  Hippocampal slices.
References:  10
mGlu3 receptor activation modulates GABA release.
Species:  Rat
Tissue:  Primary cortical neuron culture.
References:  36
It is suggested that mGlu3 receptor activation may result in the release of nerve growth factor (NGF) from rat cultured cortical astrocytes.
Species:  Rat
Tissue:  Cortical astrocytes in culture.
References:  5
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Grm3tm1Ddsc Grm3tm1Ddsc/Grm3tm1Ddsc
involves: 129S1/Sv * 129X1/SvJ * CD-1		 MGI:1351340  MP:0001362 abnormal anxiety-related response PMID: 15619115 
Grm3tm1Dgen Grm3tm1Dgen/Grm3tm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:1351340  MP:0002169 no abnormal phenotype detected
Biologically Significant Variants Click here for help
Type:  Splice variants
Species:  Human
Description:  The existence of alternatively spliced isoforms of mGlu3 has recently been reported. These are truncated forms and unequivocal expression in tissue (human brain) has been demonstrated only for GRM3Δ4, which lacks the entire transmembrane domain. Although this splice form could result in a secreted protein, immunohistochemical and fractional data showed association with the plasma membrane.
References:  24
General Comments
To date, the relative lack of mGlu3 vs. mGlu2 receptor agonists/antagonists and limited results/availability of with selective antibodies has hampered efforts to differentiate the relative roles of these two highly related receptors in the Group II mGlu receptor family.

References

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1. Brabet I, Parmentier ML, De Colle C, Bockaert J, Acher F, Pin JP. (1998) Comparative effect of L-CCG-I, DCG-IV and gamma-carboxy-L-glutamate on all cloned metabotropic glutamate receptor subtypes. Neuropharmacology, 37 (8): 1043-51. [PMID:9833633]

2. Brice NL, Varadi A, Ashcroft SJ, Molnar E. (2002) Metabotropic glutamate and GABA(B) receptors contribute to the modulation of glucose-stimulated insulin secretion in pancreatic beta cells. Diabetologia, 45 (2): 242-52. [PMID:11935156]

3. Campo B, Kalinichev M, Lambeng N, El Yacoubi M, Royer-Urios I, Schneider M, Legrand C, Parron D, Girard F, Bessif A et al.. (2011) Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression. J Neurogenet, 25 (4): 152-66. [PMID:22091727]

4. Chaki S, Yoshikawa R, Hirota S, Shimazaki T, Maeda M, Kawashima N, Yoshimizu T, Yasuhara A, Sakagami K, Okuyama S et al.. (2004) MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity. Neuropharmacology, 46 (4): 457-67. [PMID:14975669]

5. Ciccarelli R, Di Iorio P, Bruno V, Battaglia G, D'Alimonte I, D'Onofrio M, Nicoletti F, Caciagli F. (1999) Activation of A(1) adenosine or mGlu3 metabotropic glutamate receptors enhances the release of nerve growth factor and S-100beta protein from cultured astrocytes. Glia, 27 (3): 275-81. [PMID:10457374]

6. Emile L, Mercken L, Apiou F, Pradier L, Bock MD, Menager J, Clot J, Doble A, Blanchard JC. (1996) Molecular cloning, functional expression, pharmacological characterization and chromosomal localization of the human metabotropic glutamate receptor type 3. Neuropharmacology, 35 (5): 523-30. [PMID:8887960]

7. Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT et al.. (2015) Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem, 58 (18): 7485-500. [PMID:26335039]

8. Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ. (2007) A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors. J Pharmacol Exp Ther, 322 (1): 254-64. [PMID:17416742]

9. Johnson BG, Wright RA, Arnold MB, Wheeler WJ, Ornstein PL, Schoepp DD. (1999) [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology, 38 (10): 1519-29. [PMID:10530814]

10. Kew JN, Pflimlin MC, Kemp JA, Mutel V. (2002) Differential regulation of synaptic transmission by mGlu2 and mGlu3 at the perforant path inputs to the dentate gyrus and CA1 revealed in mGlu2 -/- mice. Neuropharmacology, 43 (2): 215-21. [PMID:12213275]

11. Kingston AE, Ornstein PL, Wright RA, Johnson BG, Mayne NG, Burnett JP, Belagaje R, Wu S, Schoepp DD. (1998) LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology, 37 (1): 1-12. [PMID:9680254]

12. Kuramoto T, Maihara T, Masu M, Nakanishi S, Serikawa T. (1994) Gene mapping of NMDA receptors and metabotropic glutamate receptors in the rat (Rattus norvegicus). Genomics, 19 (2): 358-61. [PMID:8188265]

13. Li ML, Yang SS, Xing B, Ferguson BR, Gulchina Y, Li YC, Li F, Hu XQ, Gao WJ. (2015) LY395756, an mGluR2 agonist and mGluR3 antagonist, enhances NMDA receptor expression and function in the normal adult rat prefrontal cortex, but fails to improve working memory and reverse MK801-induced working memory impairment. Exp Neurol, 273: 190-201. [PMID:26341392]

14. Lourenco Neto F, Schadrack J, Berthele A, Zieglgansberger W, Tolle TR, Castro-Lopes JM. (2000) Differential distribution of metabotropic glutamate receptor subtype mRNAs in the thalamus of the rat. Brain Res, 854: 93-105. [PMID:10784111]

15. Makoff A, Volpe F, Lelchuk R, Harrington K, Emson P. (1996) Molecular characterization and localization of human metabotropic glutamate receptor type 3. Brain Res Mol Brain Res, 40 (1): 55-63. [PMID:8840013]

16. Malherbe P, Knoflach F, Broger C, Ohresser S, Kratzeisen C, Adam G, Stadler H, Kemp JA, Mutel V. (2001) Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor. Mol Pharmacol, 60 (5): 944-54. [PMID:11641422]

17. Monn JA, Valli MJ, Massey SM, Hansen MM, Kress TJ, Wepsiec JP, Harkness AR, Grutsch Jr JL, Wright RA, Johnson BG et al.. (1999) Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors. J Med Chem, 42 (6): 1027-40. [PMID:10090786]

18. Muto T, Tsuchiya D, Morikawa K, Jingami H. (2007) Structures of the extracellular regions of the group II/III metabotropic glutamate receptors. Proc Natl Acad Sci USA, 104 (10): 3759-64. [PMID:17360426]

19. Nakazato A, Sakagami K, Yasuhara A, Ohta H, Yoshikawa R, Itoh M, Nakamura M, Chaki S. (2004) Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists. J Med Chem, 47 (18): 4570-87. [PMID:15317467]

20. Ohishi H, Shigemoto R, Nakanishi S, Mizuno N. (1993) Distribution of the mRNA for a metabotropic glutamate receptor (mGluR3) in the rat brain: an in situ hybridization study. J Comp Neurol, 335 (2): 252-66. [PMID:8227517]

21. Petralia RS, Wang YX, Niedzielski AS, Wenthold RJ. (1996) The metabotropic glutamate receptors, mGluR2 and mGluR3, show unique postsynaptic, presynaptic and glial localizations. Neuroscience, 71: 949-976. [PMID:8684625]

22. Petralia RS, Wang YX, Zhao HM, Wenthold RJ. (1996) Ionotropic and metabotropic glutamate receptors show unique postsynaptic, presynaptic, and glial localizations in the dorsal cochlear nucleus. J Comp Neurol, 372: 356-383. [PMID:8873866]

23. Pin JP, De Colle C, Bessis AS, Acher F. (1999) New perspectives for the development of selective metabotropic glutamate receptor ligands. Eur J Pharmacol, 375 (1-3): 277-94. [PMID:10443583]

24. Sartorius LJ, Nagappan G, Lipska BK, Lu B, Sei Y, Ren-Patterson R, Li Z, Weinberger DR, Harrison PJ. (2006) Alternative splicing of human metabotropic glutamate receptor 3. J Neurochem, 96 (4): 1139-48. [PMID:16417579]

25. Schann S, Mayer S, Franchet C, Frauli M, Steinberg E, Thomas M, Baron L, Neuville P. (2010) Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators. J Med Chem, 53 (24): 8775-9. [PMID:21105727]

26. Schoepp DD, Jane DE, Monn JA. (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology, 38 (10): 1431-76. [PMID:10530808]

27. Schweitzer C, Kratzeisen C, Adam G, Lundstrom K, Malherbe P, Ohresser S, Stadler H, Wichmann J, Woltering T, Mutel V. (2000) Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors. Neuropharmacology, 39 (10): 1700-6. [PMID:10884552]

28. Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND et al.. (2012) Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorg Med Chem Lett, 22 (12): 3921-5. [PMID:22607673]

29. Tamaru Y, Nomura S, Mizuno N, Shigemoto R. (2001) Distribution of metabotropic glutamate receptor mGluR3 in the mouse CNS: differential location relative to pre- and postsynaptic sites. Neuroscience, 106 (3): 481-503. [PMID:11591452]

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31. Tanabe Y, Nomura A, Masu M, Shigemoto R, Mizuno N, Nakanishi S. (1993) Signal transduction, pharmacological properties, and expression patterns of two rat metabotropic glutamate receptors, mGluR3 and mGluR4. J Neurosci, 13 (4): 1372-8. [PMID:8463825]

32. Wenthur CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, Daniels JS, Emmitte KA, Conn PJ, Lindsley CW. (2013) Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM). J Med Chem, 56 (12): 5208-12. [PMID:23718281]

33. Wernimont AK, Dong A, Seitova A, Crombet L, Khutoreskaya G, Edwards AM, Arrowsmith CH, Bountra C, Weigelt J, Cossar D, Dobrovetsky E, Structural Genomics Consortium (SGC). 3SM9. Accessed on 14/01/2019. Modified on 14/01/2019. http://www.rcsb.org, http://www.rcsb.org/structure/3SM9. DOI: 10.2210/pdb3SM9/pdb

34. Woltering TJ, Wichmann J, Goetschi E, Knoflach F, Ballard TM, Huwyler J, Gatti S. (2010) Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists. Bioorg Med Chem Lett, 20 (23): 6969-74. [PMID:20971004]

35. Yao Y, Pattabiraman N, Michne WF, Huang XP, Hampson DR. (2003) Molecular modeling and mutagenesis of the ligand-binding pocket of the mGlu3 subtype of metabotropic glutamate receptor. J Neurochem, 86 (4): 947-57. [PMID:12887692]

36. Zhao J, Ramadan E, Cappiello M, Wroblewska B, Bzdega T, Neale JH. (2001) NAAG inhibits KCl-induced [(3)H]-GABA release via mGluR3, cAMP, PKA and L-type calcium conductance. Eur J Neurosci, 13 (2): 340-6. [PMID:11168538]

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