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mGlu1 receptor

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Target not currently curated in GtoImmuPdb

Target id: 289

Nomenclature: mGlu1 receptor

Family: Metabotropic glutamate receptors

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 1194 6q24.3 GRM1 glutamate metabotropic receptor 1 19,32,101
Mouse 7 1199 10 A1 Grm1 glutamate receptor, metabotropic 1 125
Rat 7 1199 1p13 Grm1 glutamate metabotropic receptor 1 43,77
Previous and Unofficial Names Click here for help
GPRC1A | metabotropic glutamate receptor 1 | wobl | MGLUR1 | SCAR13 | glutamate receptor, metabotropic 1 | glutamate receptor
Database Links Click here for help
Specialist databases
GPCRDB grm1_human (Hs), grm1_mouse (Mm), grm1_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Metabotropic glutamate receptor mGluR1 complexed with LY341495 antagonist
PDB Id:  3KS9
Ligand:  LY341495
Resolution:  1.9Å
Species:  Human
References: 
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of metabotropic glutamate receptor subtype 1 complexed with glutamate
PDB Id:  1EWK
Resolution:  2.2Å
Species:  Rat
References:  56
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of metabotropic glutamate receptor subtype 1 ligand free form II
PDB Id:  1EWV
Resolution:  4.0Å
Species:  Rat
References:  56
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Metabotropic Glutamate Receptor Subtype 1 Complexed with Glutamate and Gadolinium Ion
PDB Id:  1ISR
Resolution:  4.0Å
Species:  Rat
References:  114
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Metabotropic Glutamate Receptor Subtype 1 Complexed with an antagonist
PDB Id:  1ISS
Resolution:  3.3Å
Species:  Rat
References:  114
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of metabotropic glutamate receptor subtype 1 ligand free form 1
PDB Id:  1EWT
Resolution:  3.7Å
Species:  Rat
References:  56
Image of receptor 3D structure from RCSB PDB
Description:  Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.
PDB Id:  4OR2
Ligand:  FITM
Resolution:  2.8Å
Species:  Human
References:  119
Natural/Endogenous Ligands Click here for help
L-glutamic acid
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]quisqualate Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Full agonist 7.5 – 7.7 pKd 58,71
pKd 7.5 – 7.7 [58,71]
quisqualate Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.5 – 8.0 pKi 58,83
pKi 7.5 – 8.0 [58,83]
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 – 6.5 pKi 58,83
pKi 6.4 – 6.5 [58,83]
ibotenic acid Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.9 – 6.4 pKi 83,112
pKi 5.9 – 6.4 [83,112]
(1S,3R)-ACPD Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 5.5 – 6.1 pKi 58,83,112
pKi 5.5 – 6.1 [58,83,112]
3,5-DHPG Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.8 pKi 58
pKi 5.8 [58]
L-CCG-I Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.6 pKi 83
pKi 5.6 [83]
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 4.8 – 5.0 pEC50 87
pEC50 4.8 – 5.0 [87]
(S)-3HPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 4.9 pIC50 83
pIC50 4.9 [83]
View species-specific agonist tables
Agonist Comments
Values indicated are those determined from binding studies on recombinant mGlu1a receptors. Further information on agonist pharmacology as based on functional assays can be found in [95].

So far no differences in the agonist pharmacological profile has been reported between the rat and human mGlu1 receptors using functional assays.

The best characterized agonists of the ionotropic glutamate receptors, AMPA, NMDA and kainate are inactive on mGlu1. Although several splice variants of mGlu1 have been identified (see below), all are likely to have an identical agonist pharmacology since they possess an indentical agonist binding site.

The agonist binding site is located in the large extracellular domain of this receptor, that retains its ability to bind ligands when produced as a soluble protein. The structure of this binding domain has been solved [56,114]. This domain is formed of two lobes, and agonists bind in the cleft between the two lobes. Agonists likely stabilize a closed form of this domain, whereas antagonists prevent closure. Functional importance of critical residues involved in agonist action has been confirmed by mutagenesis studies [84,93].

Cations such as Ca2+ have been proposed to directly activate mGlu1 receptors [27,55,109]. However, it is still unclear whether this is a direct agonist effect or if this is due to a potentiation of ambient glutamate produced by the cells expressing the recombinant receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AIDA Small molecule or natural product Hs Antagonist 4.2 pA2 82
pA2 4.2 [82]
[11C]JNJ-16567083 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 9.1 pKi 44
pKi 9.1 (Ki 8.7x10-10 M) [44]
LY341495 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 pKi 51
pKi 7.8 [51]
(S)-4C3HPG Small molecule or natural product Hs Antagonist 5.8 – 6.0 pKi 58,83
pKi 5.8 – 6.0 [58,83]
LY367385 Small molecule or natural product Rn Antagonist 5.9 pKi 58
pKi 5.9 (Ki 1.26x10-6 M) [58]
(S)-4CPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.4 pKi 58
pKi 5.4 [58]
DCG-IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 4.1 pKi 83
pKi 4.1 [83]
AIDA Small molecule or natural product Rn Antagonist 4.0 pKi 58
pKi 4.0 [58]
(+)-MCPG Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 3.8 pKi 58
pKi 3.8 [58]
3-MATIDA Small molecule or natural product Rn Antagonist 5.2 pIC50 81
pIC50 5.2 (IC50 6.3x10-6 M) [81]
LY367385 Small molecule or natural product Hs Antagonist 5.1 pIC50 14
pIC50 5.1 (IC50 8.8x10-6 M) [14]
(S)-TBPG Small molecule or natural product Rn Antagonist 4.2 pIC50 18
pIC50 4.2 (IC50 6.89x10-5 M) [18]
(S)-(+)-CBPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 4.2 pIC50 72
pIC50 4.2 (IC50 6.7x10-5 M) [72]
View species-specific antagonist tables
Antagonist Comments
Indicated affinities were determined by displacement studies of [3H]quisqualate bound on HEK cell membranes expressing a recombinant rat mGlu1 (except for LY341495 value determined from functional studies). More information on agonist potencies determined from functional studies can be obtained from [95]. So far no differences have been reported for the antagonist affinities between the rat and the human receptor. Although LY367385 and AIDA have been shown to specifically antagonize mGlu1 receptors versus mGlu5, both compounds are able to displace bound [3H]quisqualate to mGlu5 (see [95]).
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VU0483605 Small molecule or natural product N/A Positive 6.0 pKB 40
pKB 6.0 [40]
[3H]R214127 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 9.0 pKd 58
pKd 9.0 [58]
[3H]EM-TBPC Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Positive 8.2 pKd 71
pKd 8.2 [71]
[3H]YM298198 Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 7.5 pKd 54
pKd 7.5 (Kd 3.2x10-8 M) [54]
BAY 367620 Small molecule or natural product Rn Negative 9.5 pKi 11
pKi 9.5 (Ki 3.4x10-10 M) [11]
compound 23c [PMID: 17929793] Small molecule or natural product Rn Negative 9.4 pKi 120
pKi 9.4 (Ki 4x10-10 M) [120]
[11C]MMTP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 9.2 pKi 90
pKi 9.2 (Ki 6x10-10 M) [90]
[18F]FITM Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 9.1 pKi 121
pKi 9.1 (Ki 8.7x10-10 M) [121]
compound 11c [PMID: 17929793] Small molecule or natural product Rn Negative 9.0 pKi 120
pKi 9.0 (Ki 1x10-9 M) [120]
NPS2390 Small molecule or natural product Rn Negative 8.9 pKi 58
pKi 8.9 [58]
R214127 Small molecule or natural product Rn Negative 8.9 pKi 58
pKi 8.9 [58]
JNJ-16567083 Small molecule or natural product Rn Negative 8.9 pKi 44
pKi 8.9 (Ki 1.4x10-9 M) [44]
compound 23h [PMID: 17929793] Small molecule or natural product Rn Negative 8.8 pKi 120
pKi 8.8 (Ki 1.5x10-9 M) [120]
compound 23e [PMID: 17929793] Small molecule or natural product Rn Negative 8.8 pKi 120
pKi 8.8 (Ki 1.5x10-9 M) [120]
compound 11q [PMID: 19433355] Small molecule or natural product Rn Negative 8.5 pKi 92
pKi 8.5 (Ki 3.5x10-9 M) [92]
compound 9a [PMID: 22266036] Small molecule or natural product Hs Negative 8.4 pKi 6
pKi 8.4 (Ki 3.6x10-9 M) [6]
compound 22 [PMID: 17276684] Small molecule or natural product Hs Negative 8.4 pKi 20
pKi 8.4 (Ki 3.6x10-9 M) [20]
compound 11s [PMID: 19433355] Small molecule or natural product Rn Negative 8.3 pKi 92
pKi 8.3 (Ki 4.7x10-9 M) [92]
compound 12e [PMID: 22266036] Small molecule or natural product Rn Negative 8.3 pKi 6
pKi 8.3 (Ki 5.2x10-9 M) [6]
A-794278 Small molecule or natural product Rn Negative 8.3 pKi 124
pKi 8.3 (Ki 5.4x10-9 M) [124]
FITM Small molecule or natural product Ligand has a PDB structure Rn Negative 8.3 pKi 30
pKi 8.3 (Ki 5.4x10-9 M) [30]
Description: Measured using rat brain homogenate in a competition binding assay displacing [18F}-FITM.
compound 27 [PMID: 20346665] Small molecule or natural product Rn Negative 8.1 pKi 91
pKi 8.1 (Ki 7.9x10-9 M) [91]
compound 29 [PMID: 17064898] Small molecule or natural product Rn Negative 8.0 pKi 86
pKi 8.0 (Ki 9.3x10-9 M) [86]
FPTQ Small molecule or natural product Rn Negative 7.9 pKi 29
pKi 7.9 (Ki 1.26x10-8 M) [29]
EM-TBPC Small molecule or natural product Rn Negative 7.8 pKi 71
pKi 7.8 (Ki 1.7x10-8 M) [71]
Ro67-7476 Small molecule or natural product Rn Positive 7.5 – 7.9 pKi 52
pKi 7.5 – 7.9 (Ki 3.16x10-8 – 1.26x10-8 M) [52]
YM-202074 Small molecule or natural product Rn Negative 7.7 pKi 53
pKi 7.7 (Ki 2x10-8 M) [53]
Ro01-6128 Small molecule or natural product Rn Positive 7.5 – 7.7 pKi 52
pKi 7.5 – 7.7 (Ki 3.16x10-8 – 1.99x10-8 M) [52]
compound 24 [PMID: 20346665] Small molecule or natural product Hs Negative 6.9 pKi 91
pKi 6.9 (Ki 1.15x10-7 M) [91]
compound 24 [PMID: 20346665] Small molecule or natural product Rn Negative 6.9 pKi 91
pKi 6.9 (Ki 1.15x10-7 M) [91]
compound 2f [PMID: 17532216] Small molecule or natural product Hs Negative 6.9 pKi 118
pKi 6.9 (Ki 1.27x10-7 M) [118]
LY456066 Small molecule or natural product Rn Negative 6.8 pKi 31
pKi 6.8 (Ki 1.43x10-7 M) [31]
CPCCOEt Small molecule or natural product Click here for species-specific activity table Rn Negative 5.3 pKi 58
pKi 5.3 [58]
Ro67-4853 Small molecule or natural product Rn Positive 5.1 pKi 52
pKi 5.1 (Ki 7.94x10-6 M) [52]
Ro0711401 Small molecule or natural product Rn Positive 7.3 pEC50 117
pEC50 7.3 (EC50 5.6x10-8 M) [117]
compound 3a [PMID: 16099654] Small molecule or natural product Rn Positive 7.2 pEC50 116
pEC50 7.2 (EC50 6.5x10-8 M) [116]
compound 4b [PMID: 16099654] Small molecule or natural product Rn Positive 7.2 pEC50 116
pEC50 7.2 (EC50 6.5x10-8 M) [116]
VU0483605 Small molecule or natural product Hs Positive 6.4 pEC50 12
pEC50 6.4 (EC50 3.9x10-7 M) [12]
VU-71 Small molecule or natural product Rn Positive 5.6 pEC50 116
pEC50 5.6 (EC50 2.4x10-6 M) [116]
CPCCOEt Small molecule or natural product Click here for species-specific activity table Rn Negative 5.3 pEC50 59
pEC50 5.3 (EC50 5x10-6 M) [59]
compound 11q [PMID: 19433355] Small molecule or natural product Hs Negative 9.1 pIC50 92
pIC50 9.1 (IC50 9x10-10 M) [92]
A-841720 Small molecule or natural product Rn Negative 9.0 – 9.0 pIC50 123-124
pIC50 9.0 – 9.0 (IC50 1.05x10-9 – 1x10-9 M) [123-124]
JNJ16259685 Small molecule or natural product Hs Negative 8.9 pIC50 62
pIC50 8.9 (IC50 1.21x10-9 M) [62]
compound 23i [PMID: 17929793] Small molecule or natural product Hs Negative 8.9 pIC50 120
pIC50 8.9 (IC50 1.4x10-9 M) [120]
compound 24 [PMID: 20346665] Small molecule or natural product Hs Negative 8.7 pIC50 91
pIC50 8.7 (IC50 2.1x10-9 M) [91]
compound 11s [PMID: 19433355] Small molecule or natural product Hs Negative 8.7 pIC50 92
pIC50 8.7 (IC50 2.1x10-9 M) [92]
compound 23h [PMID: 17929793] Small molecule or natural product Hs Negative 8.7 pIC50 120
pIC50 8.7 (IC50 2.2x10-9 M) [120]
compound 23c [PMID: 17929793] Small molecule or natural product Hs Negative 8.6 pIC50 120
pIC50 8.6 (IC50 2.5x10-9 M) [120]
CFMTI Small molecule or natural product Hs Negative 8.6 pIC50 94
pIC50 8.6 (IC50 2.6x10-9 M) [94]
compound 23e [PMID: 17929793] Small molecule or natural product Hs Negative 8.5 pIC50 120
pIC50 8.5 (IC50 2.9x10-9 M) [120]
A-794282 Small molecule or natural product Hs Negative 8.5 pIC50 122
pIC50 8.5 (IC50 3x10-9 M) [122]
compound 22 [PMID: 19289283] Small molecule or natural product Rn Negative 8.5 pIC50 73
pIC50 8.5 (IC50 3x10-9 M) [73]
[18F]MK-1312 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 8.4 pIC50 42
pIC50 8.4 (IC50 3.6x10-9 M) [42]
MK-5435 Small molecule or natural product Hs Negative 8.4 pIC50 42
pIC50 8.4 (IC50 4.3x10-9 M) [42]
A-794282 Small molecule or natural product Rn Negative 8.3 pIC50 124
pIC50 8.3 (IC50 4.7x10-9 M) [124]
FTIDC Small molecule or natural product Rn Negative 8.3 pIC50 105
pIC50 8.3 (IC50 4.8x10-9 M) [105]
compound 11c [PMID: 17929793] Small molecule or natural product Hs Negative 8.3 pIC50 120
pIC50 8.3 (IC50 4.9x10-9 M) [120]
[18F]FITM Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 8.3 pIC50 121
pIC50 8.3 (IC50 5.1x10-9 M) [121]
[18F]FPIT Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 8.3 pIC50 28
pIC50 8.3 (IC50 5.4x10-9 M) [28]
FTIDC Small molecule or natural product Hs Negative 8.2 pIC50 105
pIC50 8.2 (IC50 5.8x10-9 M) [105]
compound 32 [PMID: 19289283] Small molecule or natural product Rn Negative 8.2 pIC50 73
pIC50 8.2 (IC50 6x10-9 M) [73]
compound 10i [PMID: 23084894] Small molecule or natural product Hs Negative 8.2 pIC50 10
pIC50 8.2 (IC50 6x10-9 M) [10]
compound 9a [PMID: 22266036] Small molecule or natural product Hs Negative 8.2 pIC50 6
pIC50 8.2 (IC50 6.3x10-9 M) [6]
compound 9n [PMID: 23084894] Small molecule or natural product Hs Negative 8.1 pIC50 10
pIC50 8.1 (IC50 7x10-9 M) [10]
YM-202074 Small molecule or natural product Rn Negative 8.1 pIC50 53
pIC50 8.1 (IC50 8.6x10-9 M) [53]
compound 29 [PMID: 17064898] Small molecule or natural product Rn Negative 8.1 pIC50 86
pIC50 8.1 (IC50 9x10-9 M) [86]
[11C]MMTP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 8.0 pIC50 90
pIC50 8.0 (IC50 9.5x10-9 M) [90]
A-841720 Small molecule or natural product Hs Negative 8.0 pIC50 122
pIC50 8.0 (IC50 1x10-8 M) [122]
A-794278 Small molecule or natural product Hs Negative 8.0 pIC50 122
pIC50 8.0 (IC50 1x10-8 M) [122]
R214127 Small molecule or natural product Hs Negative 8.0 pIC50 58
pIC50 8.0 (IC50 1.04x10-8 M) [58]
compound 12e [PMID: 22266036] Small molecule or natural product Hs Negative 7.9 pIC50 6
pIC50 7.9 (IC50 1.2x10-8 M) [6]
DM-PPP Small molecule or natural product Rn Negative 7.8 pIC50 80
pIC50 7.8 [80]
YM298198 Small molecule or natural product Rn Negative 7.8 pIC50 54
pIC50 7.8 [54]
3,5-dimethyl PPP Small molecule or natural product Rn Negative 7.8 pIC50 80
pIC50 7.8 (IC50 1.58x10-8 M) [80]
compound 3 [PMID: 12470711] Small molecule or natural product Rn Negative 7.8 pIC50 80
pIC50 7.8 (IC50 1.6x10-8 M) [80]
compound 27 [PMID: 20346665] Small molecule or natural product Hs Negative 7.6 pIC50 91
pIC50 7.6 (IC50 2.7x10-8 M) [91]
LY456066 Small molecule or natural product Hs Negative 7.6 pIC50 31
pIC50 7.6 (IC50 2.8x10-8 M) [31]
BAY 367620 Small molecule or natural product Rn Negative 6.8 – 8.0 pIC50 11,58
pIC50 6.8 – 8.0 (IC50 1.58x10-7 – 1x10-8 M) [11,58]
A-850002 Small molecule or natural product Rn Negative 7.4 pIC50 124
pIC50 7.4 (IC50 4.09x10-8 M) [124]
A-850002 Small molecule or natural product Hs Negative 7.4 pIC50 122
pIC50 7.4 (IC50 4.3x10-8 M) [122]
CFMMC Small molecule or natural product Hs Negative 7.3 pIC50 31
pIC50 7.3 (IC50 5x10-8 M) [31]
cis-10 [PMID: 15771457] Small molecule or natural product Hs Negative 7.0 pIC50 69
pIC50 7.0 (IC50 9.4x10-8 M) [69]
VU0469650 Small molecule or natural product Hs Negative 7.0 pIC50 66
pIC50 7.0 (IC50 9.9x10-8 M) [66]
YM298198 Small molecule or natural product Hs Negative 6.9 pIC50 31
pIC50 6.9 (IC50 1.2x10-7 M) [31]
LY456236 Small molecule or natural product Hs Negative 6.9 pIC50 64
pIC50 6.9 (IC50 1.4x10-7 M) [64]
EM-TBPC Small molecule or natural product Rn Negative 6.9 pIC50 71
pIC50 6.9 (IC50 1.28x10-7 M) [71]
compound 22 [PMID: 17276684] Small molecule or natural product Rn Negative 6.8 pIC50 20
pIC50 6.8 (IC50 1.67x10-7 M) [20]
CPCCOEt Small molecule or natural product Hs Negative 5.2 – 5.8 pIC50 65
pIC50 5.2 – 5.8 (IC50 6.3x10-6 – 1.5x10-6 M) [65]
PHCCC Small molecule or natural product Click here for species-specific activity table Hs Positive - -
View species-specific allosteric modulator tables
Allosteric Modulator Comments
Values for Ro67-4853 and Ro67-7476 were determined by binding studies using [3H]R214127 binding [58] or from functional studies [11,52,65]. Among these allosteric regulators only NPS2390 is not mGlu1 selective, being also active as a negative allosteric modulator of mGlu5. Among the positive modulators, only Ro67-4853 is active on the human receptor [52]. The binding site of all allosteric regulators have been mapped within the 7 transmembrane domain of the receptor [11,52,65,71].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Comments:  The primary action of the mGlu1 is to activate PLC through stimulating Gq/11, resulting in the PIP2 breakdown which can be monitored as the production of inositol phosphate. The PIP2 breakdown causes the increases in the intracellular calcium concentration and the activation of the TRPC channels [38]. The primary transduction is observed both in cell lines and the native tissue expressing the mGlu1.
References:  3,16,24,88
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family
Gi/Go family
G protein independent mechanism
Adenylate cyclase stimulation
Adenylate cyclase inhibition
Phospholipase A2 stimulation
Phospholipase D stimulation
Other - See Comments
Comments:  Stimulation of adenylyl cyclase via mGlu1 has been reported in transfected cell lines [24] and suggested in neuronal cells [104]. Activation of the mGlu1 triggers the PTX-sensitive Gi/o signaling pathway in transfected cell lines, but its physiological role is unclear. The mGlu1 also induces the phospohrylation of the ERK in the G protein dependent and independent manner. In the latter case, the effects are mediated via beta-arrestin and dependent on the type of the ligands [22]. Activation of PLD has been reported in a cell line and native tissues [24,96]. The mGlu1 has been reported to activate the TRPC1 channels indepedently of G protein [50].
References:  3,16,24,88
Tissue Distribution Click here for help
Testes.
Species:  Human
Technique:  immunocytochemistry.
References:  103
Thymus, thymocytes, TC-1s thymic epithelial cell line.
Species:  Mouse
Technique:  RT-PCR.
References:  102
Peripheral unmyelinated sensory afferent terminals.
Species:  Mouse
Technique:  Immunoelectron microscopy.
References:  8
At the subcellular level, mGlu1 proteins were found in post-synaptic elements on the side of the post-synaptic density. Although some reports have suggested the presence of mGlu1 in pre-synaptic elements, this issue remains at present unresolved.
Species:  Rat
Technique:  immunocytochemistry.
References:  26,67-68
Olfactory bulb, stratum oriens of CA1 and polymorph layer of dentate gyrus in hippocampus, globus pallidus, thalamus, substantia nigra, superior colliculus, cerebellum > neocortex, striatum, amygdala, hypothalamus, medulla.
Species:  Rat
Technique:  Immunohistochemistry.
References:  74
GABAergic neurons of the cerebellar cortex, somatostatin/GABA-immunopositive cells in the neocortex and hippocampus.
Species:  Rat
Technique:  Immunohistochemistry.
References:  5
Olfactory bulb, CA3 region of the hippocampus, dentate gyrus, globus pallidus, thalamic nuclei, medial geniculate nucleus, mammillary bodies, Darkshevich's nucleus, deep cerebellar nuclei, lateral vestibular nucleus, facial nucleus, spinal motor nucleus of the trigeminal nerve.
Species:  Rat
Technique:  in situ hybridisation.
References:  26
Olfactory bulb, thalamic nuclei (anterodorsal, anteroventral, ventrolateral posterior, medial geniculate, nucleus gelatinosum) > lateral hypothalamus, island of Calleja, mammillary bodies, nucleus of Darkshevich, brainstem, cranial nuclei, ventral horn of the spinal cord.
Species:  Rat
Technique:  Immunohistochemistry.
References:  26
mGlu1(a): cerebellum, diencephalon, mesencephalon, olfactory bulb, brainstem.
mGlu1(b): cerebral cortex, septum, striatum.
Species:  Rat
Technique:  PCR.
References:  37
In the hippocampus, mGlu1(a) is located in non-principal neurones in all areas, including the oriens-alveus border of the CA1 field, whereas mGlu1(b) is expressed in principal cells of the CA3 field and dentate granule cells, but absent in the CA1 region.
Species:  Rat
Technique:  Immunohistochemistry.
References:  23
Purkinje cell bodies and dendrites, golgi neurones of the granular cell layer, hippocampus (interneurons of the striatum oriens and dentate hilar region).
Species:  Rat
Technique:  immunocytochemistry.
References:  37
mGlu1(b): magnocellular neurons of the neuroendocrine supraoptic, paraventricular and circuate nuclei, neuronal cell bodies of the retrochiasmatic, anterior commissural and paraventricular nuclei.
Species:  Rat
Technique:  immunocytochemistry.
References:  78
mGlu1(b) and mGlu1(c): Hippocampus: CA3 region > granule cells.
Absent in CA1 region.
Species:  Rat
Technique:  Immunohistochemistry.
References:  67
mGlu1(a): heart: nerve terminals, ganglion cells and elements of the conducting system.
Species:  Rat
Technique:  immunocytochemistry.
References:  34
Subpopulation of basal keratinocytes.
Species:  Rat
Technique:  immunocytochemistry.
References:  33
mGlu1(a) and mGlu1(b): circumvallate papillae (taste buds).
Species:  Rat
Technique:  RT-PCR, in situ hybridisation, immunocytochemistry.
References:  113
Hippocampal dentate gyrus and CA2-3, cerebellar Purkinje cells.
Species:  Rat
Technique:  in situ hybridization.
References:  77
When examined at the electron microscopic level in the cerebellar cortex, mGlu(1b) was found at the same perisynaptic location as mGlu(1a).
Species:  Rat
Technique:  immunocytochemistry.
References:  79
Cerebellum, mitral and tufted cells of the olfactory bulb, hippocampus, lateral septum, thalamus, globus pallidus, entopendenuclear nucleus, ventral pallidum, magnocellular preoptic nucleus, substantia nigra, dorsal cochlear nucleus > dentate gyrus, striatum, islands of Calleja, superficial layers of the retrospinal, cingulate and entorhinal cortices, mammillary nuclei, red nucleus, superior colliculus.
Species:  Rat
Technique:  in situ hybridization.
References:  98
Cerebellar cortex.
Species:  Rat
Technique:  immunocytochemistry.
References:  45
Neostriatum, neocortex, hippocampus.
Species:  Rat
Technique:  in situ hybridization.
References:  49
Unipolar brush cells of cerebellum and cochlear nuclear complex.
Species:  Rat
Technique:  immunocytochemistry.
References:  47
Striatal neurons.
Species:  Rat
Technique:  Immunohistochemistry.
References:  107
Retina.
Species:  Rat
Technique:  in situ hybridisation.
References:  39
Cerebellum, thalamus, dentate gyrus, medial central gray > CA3 region of the hippocampus and hypothalamus > basal ganglia, cortex.
Species:  Rat
Technique:  Radioligand binding.
References:  60
Testes.
Species:  Rat
Technique:  RT-PCR.
References:  103
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
Measurement of IP levels
Species:  Rat
Tissue:  HEK 293 cells
Response measured:  IP accumulation
References:  75
Measurement of IP levels in CHO cells transfected with the rat mGlu1.
Species:  Rat
Tissue:  CHO cells.
Response measured:  IP formation.
References:  97
Measurement of Ca2+ levels in CHO cells transfected with the rat mGlu1 receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Ca2+ mobilisation.
References:  62
Measurement of IP levels in rat cerebellar granule cells expressing the native mGlu1 receptor.
Species:  Rat
Tissue:  Primary cultures of cerebellar granule cells.