Top ▲

GluA1

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 444

Nomenclature: GluA1

Family: Ionotropic glutamate receptors

Gene and Protein Information Click here for help
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 906 5q33.2 GRIA1 glutamate ionotropic receptor AMPA type subunit 1 5-6,9
Mouse 3 1 907 11 B1.3 Gria1 glutamate receptor, ionotropic, AMPA1 (alpha 1) 7
Rat 3 1 907 10 Gria1 glutamate ionotropic receptor AMPA type subunit 1 1-2,8
Previous and Unofficial Names Click here for help
GluRA | HBGR1 | AMPA-selective glutamate receptor 1 | gluR-1 | glutamate receptor subunit GluR1 | Glr1 | HIPA1 | glutamate receptor
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
L-glutamic 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
(S)-5-fluorowillardiine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
[3H]AMPA Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist - -
AMPA Small molecule or natural product Click here for species-specific activity table Hs Full agonist - -
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]CNQX Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
ATPO Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
GYKI53655 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
GYKI53784 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
active isomer, non-competitive
tezampanel Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
NBQX Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
extracellular argiotoxin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - no - - - no

Not voltage dependent
extracellular joro toxin Small molecule or natural product Click here for species-specific activity table Hs - no - - - no
selective for channels lacking GluA2
Not voltage dependent
Channel Blocker Comments
GluA1 is also blocked by intracellular polyamines.
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
LY392098 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.8 pEC50 - no 3
pEC50 5.8 (EC50 1.77x10-6 M) [3]
Not voltage dependent
LY404187 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.3 pEC50 - no 3
pEC50 5.3 (EC50 5.65x10-6 M) [3]
Not voltage dependent
cyclothiazide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Positive 4.7 pEC50 - no 3
pEC50 4.7 (EC50 1.9x10-5 M) [3]
Not voltage dependent
aniracetam Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Positive - - - no

Not voltage dependent
CX516 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Positive - - - no

Not voltage dependent
CX546 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
IDRA-21 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
LY503430 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
piracetam Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Positive - - - no

Not voltage dependent
S18986 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
Allosteric Modulator Comments
Piracetam and aniracetam are examples of pyrrolidinones. Cyclothiazide, S18986, and IDRA-21 are examples of benzothiadiazides. CX516 and CX546 are examples of benzylpiperidines. LY392098, LY404187 and LY503430 are examples of biarylpropylsulfonamides.
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0031623 receptor internalization IEA
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Rat
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  1-2,8
Type:  Splice variant
Species:  Mouse
Description:  ‘flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  7
Type:  Splice variant
Species:  Mouse
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  7
Type:  Splice variant
Species:  Human
Description:  ‘flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  4-6,9
Type:  Splice variant
Species:  Human
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  5-6,9
Biologically Significant Variant Comments
GluA1 exists as alternatively spliced ‘flip’ and ‘flop’ isoforms which differ with respect to a cassette of 35 amino acids in the extracellular loop between M3 and M4 [2,8]. Tetrameric receptors assembled from the ‘flop’ isoform recover from desensitization at a slower rate than those formed from the ‘flip’ isoform, but have comparable rates of desensitization onset [4].

References

Show »

1. Hollmann M, O'Shea-Greenfield A, Rogers SW, Heinemann S. (1989) Cloning by functional expression of a member of the glutamate receptor family. Nature, 342 (6250): 643-8. [PMID:2480522]

2. Keinänen K, Wisden W, Sommer B, Werner P, Herb A, Verdoorn TA, Sakmann B, Seeburg PH. (1990) A family of AMPA-selective glutamate receptors. Science, 249 (4968): 556-60. [PMID:2166337]

3. Miu P, Jarvie KR, Radhakrishnan V, Gates MR, Ogden A, Ornstein PL, Zarrinmayeh H, Ho K, Peters D, Grabell J et al.. (2001) Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology, 40 (8): 976-83. [PMID:11406188]

4. Mosbacher J, Schoepfer R, Monyer H, Burnashev N, Seeburg PH, Ruppersberg JP. (1994) A molecular determinant for submillisecond desensitization in glutamate receptors. Science, 266 (5187): 1059-62. [PMID:7973663]

5. Potier MC, Spillantini MG, Carter NP. (1992) The human glutamate receptor cDNA GluR1: cloning, sequencing, expression and localization to chromosome 5. DNA Seq., 2 (4): 211-8. [PMID:1320959]

6. Puckett C, Gomez CM, Korenberg JR, Tung H, Meier TJ, Chen XN, Hood L. (1991) Molecular cloning and chromosomal localization of one of the human glutamate receptor genes. Proc. Natl. Acad. Sci. U.S.A., 88 (17): 7557-61. [PMID:1652753]

7. Sakimura K, Bujo H, Kushiya E, Araki K, Yamazaki M, Yamazaki M, Meguro H, Warashina A, Numa S, Mishina M. (1990) Functional expression from cloned cDNAs of glutamate receptor species responsive to kainate and quisqualate. FEBS Lett., 272 (1-2): 73-80. [PMID:1699805]

8. Sommer B, Keinänen K, Verdoorn TA, Wisden W, Burnashev N, Herb A, Köhler M, Takagi T, Sakmann B, Seeburg PH. (1990) Flip and flop: a cell-specific functional switch in glutamate-operated channels of the CNS. Science, 249 (4976): 1580-5. [PMID:1699275]

9. Sun W, Ferrer-Montiel AV, Schinder AF, McPherson JP, Evans GA, Montal M. (1992) Molecular cloning, chromosomal mapping, and functional expression of human brain glutamate receptors. Proc. Natl. Acad. Sci. U.S.A., 89 (4): 1443-7. [PMID:1311100]

Contributors

Show »

How to cite this page