Nomenclature: GluA3

Family: Ionotropic glutamate receptors

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

Contents

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 894 Xq25-q26 GRIA3 glutamate receptor, ionotropic, AMPA 3 2,6,9
Mouse 3 1 888 X A3.3-A4 Gria3 glutamate receptor, ionotropic, AMPA3 (alpha 3) 10,12
Rat 3 1 888 Xq11 Gria3 glutamate receptor, ionotropic, AMPA 3 1,3,8,11
Previous and Unofficial Names
GLUA3
GluR3
GluRC
GluR-C
GluR-K3
MRX94
glutamate receptor, ionotrophic, AMPA 3
GluR-3
AMPA-selective glutamate receptor 3
glutamate receptor 3
glutamate receptor, ionotropic, AMPA3 (alpha 3)
Gluralpha3
2900064I19Rik
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
Orphanet Gene
PharmGKB Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligand(s)
L-glutamic acid
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AMPA Hs Full agonist - -
(S)-5-fluorowillardiine Hs Full agonist - -
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
GYKI53655 Hs Antagonist - -
tezampanel Hs Antagonist - -
GYKI53784 Hs Antagonist - -
active isomer, non-competitive
ATPO 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
Allosteric Regulators
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
aniracetam Hs Positive - - - no

Not voltage dependent
LY392098 Hs Positive - - - no

Not voltage dependent
CX516 Hs Positive - - - no

Not voltage dependent
S18986 Hs Positive - - - no

Not voltage dependent
cyclothiazide Hs Positive - - - no

Not voltage dependent
LY404187 Hs Positive - - - no

Not voltage dependent
LY503430 Hs Positive - - - no

Not voltage dependent
piracetam Hs Positive - - - no

Not voltage dependent
CX546 Hs Positive - - - no

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

Not voltage dependent
Clinically-Relevant Mutations and Pathophysiology
Disease:  X-linked syndromic intellectual deficit Wu type
OMIM:  300699
Orphanet:  364028
References: 
Mutations not determined
Biologically Significant Variants
Type:  Splice variant.
Species:  Mouse
Description:  ‘flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  10,12
Type:  Splice variant.
Species:  Human
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  2,6,9
Type:  Splice variant.
Species:  Human
Description:  ‘flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  2,6,9
Type:  Splice variant.
Species:  Rat
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  1,3,8,11
Type:  Splice variant.
Species:  Rat
Description:  'flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  1,3,8,11
Biologically Significant Variant Comments
GluA3 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 [3,11]. Tetrameric receptors assembled from the ‘flip’ isoform enter the desensitized state more slowly, and recover more quickly, than those formed from the ‘flop’ isoform [4,7]. RNA editing (AGA->IGA) occurs at a codon for arginine (unedited), or glycine (edited) at a locus with the extracellular loop that immediately precedes the alternatively spliced ‘flip’ and ‘flop’ modules. Edited channels recover from desensitization at a faster rate than those that are unedited [5].

REFERENCES

1. Boulter J, Hollmann M, O'Shea-Greenfield A, Hartley M, Deneris E, Maron C, Heinemann S. (1990) Molecular cloning and functional expression of glutamate receptor subunit genes. Science249 (4972): 1033-7. [PMID:2168579]

2. Hollmann M, Hartley M, Heinemann S. (1991) Ca2+ permeability of KA-AMPA--gated glutamate receptor channels depends on subunit composition. Science252 (5007): 851-3. [PMID:1709304]

3. Keinänen K, Wisden W, Sommer B, Werner P, Herb A, Verdoorn TA, Sakmann B, Seeburg PH. (1990) A family of AMPA-selective glutamate receptors. Science249 (4968): 556-60. [PMID:2166337]

4. Koike M, Tsukada S, Tsuzuki K, Kijima H, Ozawa S. (2000) Regulation of kinetic properties of GluR2 AMPA receptor channels by alternative splicing. J. Neurosci.20 (6): 2166-74. [PMID:10704491]

5. Lomeli H, Mosbacher J, Melcher T, Höger T, Geiger JR, Kuner T, Monyer H, Higuchi M, Bach A, Seeburg PH. (1994) Control of kinetic properties of AMPA receptor channels by nuclear RNA editing. Science266 (5191): 1709-13. [PMID:7992055]

6. McNamara JO, Eubanks JH, McPherson JD, Wasmuth JJ, Evans GA, Heinemann SF. (1992) Chromosomal localization of human glutamate receptor genes. J. Neurosci.12 (7): 2555-62. [PMID:1319477]

7. Mosbacher J, Schoepfer R, Monyer H, Burnashev N, Seeburg PH, Ruppersberg JP. (1994) A molecular determinant for submillisecond desensitization in glutamate receptors. Science266 (5187): 1059-62. [PMID:7973663]

8. Nakanishi N, Shneider NA, Axel R. (1990) A family of glutamate receptor genes: evidence for the formation of heteromultimeric receptors with distinct channel properties. Neuron5 (5): 569-81. [PMID:1699567]

9. Rampersad V, Elliott CE, Nutt SL, Foldes RL, Kamboj RK. (1994) Human glutamate receptor hGluR3 flip and flop isoforms: cloning and sequencing of the cDNAs and primary structure of the proteins. Biochim. Biophys. Acta1219 (2): 563-6. [PMID:7918660]

10. Sakimura K, Morita T, Kushiya E, Mishina M. (1992) Primary structure and expression of the gamma 2 subunit of the glutamate receptor channel selective for kainate. Neuron8 (2): 267-74. [PMID:1310861]

11. 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. Science249 (4976): 1580-5. [PMID:1699275]

12. Sommer B, Köhler M, Sprengel R, Seeburg PH. (1991) RNA editing in brain controls a determinant of ion flow in glutamate-gated channels. Cell67 (1): 11-9. [PMID:1717158]

To cite this database page, please use the following:

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluA3. Last modified on 17/03/2014. Accessed on 18/04/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=446.

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