GluA1 | Ionotropic glutamate receptors | IUPHAR/BPS Guide to PHARMACOLOGY

GluA1

Target id: 444

Nomenclature: GluA1

Family: Ionotropic glutamate receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GluA1 in GtoImmuPdb

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 906 5q31.1 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
GluRA | HBGR1 | AMPA-selective glutamate receptor 1 | gluR-1 | glutamate receptor subunit GluR1 | Glr1 | HIPA1 | glutamate receptor
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
L-glutamic acid

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
(S)-5-fluorowillardiine Hs Full agonist - -
[3H]AMPA Hs Full agonist - -
AMPA Hs Full agonist - -
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]CNQX Hs Antagonist - -
ATPO Hs Antagonist - -
GYKI53655 Hs Antagonist - -
GYKI53784 Hs Antagonist - -
active isomer, non-competitive
tezampanel Hs Antagonist - -
NBQX Hs Antagonist - -
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
extracellular argiotoxin Hs - no - - - no

Not voltage dependent
extracellular joro toxin 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 Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
LY392098 Hs Positive 5.8 pEC50 - no 3
pEC50 5.8 (EC50 1.77x10-6 M) [3]
Not voltage dependent
LY404187 Hs Positive 5.3 pEC50 - no 3
pEC50 5.3 (EC50 5.65x10-6 M) [3]
Not voltage dependent
cyclothiazide Hs Positive 4.7 pEC50 - no 3
pEC50 4.7 (EC50 1.9x10-5 M) [3]
Not voltage dependent
aniracetam Hs Positive - - - no

Not voltage dependent
CX516 Hs Positive - - - no

Not voltage dependent
CX546 Hs Positive - - - no

Not voltage dependent
IDRA-21 Hs Positive - - - no

Not voltage dependent
LY503430 Hs Positive - - - no

Not voltage dependent
piracetam Hs Positive - - - no

Not voltage dependent
S18986 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.
Biologically Significant Variants
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

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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

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How to cite this page

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluA1. Last modified on 25/06/2015. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=444.