Nomenclature: GluN2A

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 1464 16p13.2 GRIN2A glutamate receptor, ionotropic, N-methyl D-aspartate 2A
Mouse 3 1 1464 16 A1 Grin2a glutamate receptor, ionotropic, NMDA2A (epsilon 1)
Rat 3 1 1464 10q11 Grin2a glutamate receptor, ionotropic, N-methyl D-aspartate 2A
Previous and Unofficial Names
GLUN2A
NMDA-R2A
NR2A
GluRε1
NMDAR2A
N-methyl D-aspartate receptor subtype 2A
N-methyl-D-aspartate receptor subunit 2A
glutamate [NMDA] receptor subunit epsilon-1
GluRepsilon1
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 Ligands
L-glutamic acid
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
D-aspartate Hs Agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
homoquinolinic acid Hs Full agonist - -
[Binds to: glutamate site] GluN2B ≥ GluN2A ≥ GluN2D > GluN2C; partial agonist at GluN2A and GluN2C
glycine Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
D-serine Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
[3H]glycine Hs Agonist - -
[Binds to: glycine site]
(+)-HA966 Hs Partial agonist - -
[Binds to: glycine site] GluN2B > GluN2A
NMDA Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C > GluN2B > GluN2A
(RS)-(tetrazol-5-yl)glycine Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
L-aspartate Hs Agonist - -
[Binds to: glutamate site] GluN2D = GluN2B > GluN2C = GluN2A
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
UBP141 Hs Antagonist - - 4
[Binds to: glutamate site] GluN2D ≥ GluN2C > GluN2A ≥ GluN2B [4]
LY233053 Hs Antagonist - -
[Binds to: glutamate site]
NVP-AAM077 Hs Antagonist - - 1-3,5
[Binds to: glutamate site] GluN2A > GluN2B (human), but weakly selective for rat GluN2A versus GluN2B [1-3,5]
selfotel Hs Antagonist - -
[Binds to: glutamate site]
L701324 Hs Antagonist - -
[Binds to: glycine site]
CGP37849 Hs Antagonist - -
[Binds to: glutamate site]
conantokin-G Hs Antagonist - -
[Binds to: glutamate site] GluN2B > GluN2D = GluN2C = GluN2A
d-CCPene Hs Antagonist - -
[Binds to: glutamate site] GluN2A = GluN2B > GluN2C = GluN2D
[3H]CGP39653 Hs Antagonist - -
[Binds to: glutamate site]
d-AP5 Hs Antagonist - -
[Binds to: glutamate site]
[3H]L689560 Hs Antagonist - -
[Binds to: glycine site]
GV196771A Hs Antagonist - -
[Binds to: glycine site]
[3H]CGP61594 Hs Antagonist - -
[Binds to: glycine site] [3H]CGP61594 is a photoaffinity ligand
[3H]CGS19755 Hs Antagonist - -
[Binds to: glutamate site]
[3H]CPP Hs Antagonist - -
[Binds to: glutamate site]
L689560 Hs Antagonist - -
[Binds to: glycine site]
[3H]MDL105519 Hs Antagonist - -
[Binds to: glycine site]
5,7-dichlorokynurenic acid Hs Antagonist - -
[Binds to: glycine site]
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
memantine Hs - no - - - no
GluN2C ≥ GluN2D ≥ GluN2B > GluN2A
Not voltage dependent
dizocilpine Hs - no - - - no

Not voltage dependent
phencyclidine Hs - no - - - no

Not voltage dependent
Mg2+ Hs - no - - - no
GluN2A = GluN2B > GluN2C = GluN2D
Not voltage dependent
amantidine Hs - no - - - no
GluN2C = GluN2D ≥ GluN2B ≥ GluN2A
Not voltage dependent
[3H]MK-801 Hs - no - - - no
[Binds to: cation channel]
Not voltage dependent
N1-dansyl-spermine Hs - no - - - no
GluN2A = GluN2B >> GluN2C = GluN2D
Not voltage dependent
ketamine Hs - no - - - no

Not voltage dependent
Clinically-Relevant Mutations and Pathophysiology
Disease:  Epilepsy, focal, with speech disorder and with or without mental retardation
OMIM:  245570
Orphanet:  289266, 98818
References: 
Mutations not determined
Disease:  Rolandic epilepsy, mental retardation, and speech dyspraxia
OMIM:  300643, 245570
Orphanet:  163721
References: 
Mutations not determined
Disease:  Epileptic encephalopathy with continuous spike-and-wave during sleep
Orphanet:  725
References: 
Mutations not determined
Disease:  Benign familial epilepsy of childhood with rolandic spikes
OMIM:  245570
Orphanet:  1945
References: 
Mutations not determined

REFERENCES

1. Auberson YP, Allgeier H, Bischoff S, Lingenhoehl K, Moretti R, Schmutz M. (2002) 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorg. Med. Chem. Lett.12 (7): 1099-102. [PMID:11909726]

2. Feng B, Tse HW, Skifter DA, Morley R, Jane DE, Monaghan DT. (2004) Structure-activity analysis of a novel NR2C/NR2D-preferring NMDA receptor antagonist: 1-(phenanthrene-2-carbonyl) piperazine-2,3-dicarboxylic acid. Br. J. Pharmacol.141 (3): 508-16. [PMID:14718249]

3. Frizelle PA, Chen PE, Wyllie DJ. (2006) Equilibrium constants for (R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-methyl]-phosphonic acid (NVP-AAM077) acting at recombinant NR1/NR2A and NR1/NR2B N-methyl-D-aspartate receptors: Implications for studies of synaptic transmission. Mol. Pharmacol.70 (3): 1022-32. [PMID:16778008]

4. Morley RM, Tse HW, Feng B, Miller JC, Monaghan DT, Jane DE. (2005) Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists. J. Med. Chem.48 (7): 2627-37. [PMID:15801853]

5. Neyton J, Paoletti P. (2006) Relating NMDA receptor function to receptor subunit composition: limitations of the pharmacological approach. J. Neurosci.26 (5): 1331-3. [PMID:16452656]

To cite this database page, please use the following:

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluN2A. Last modified on 18/03/2014. Accessed on 21/08/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=456.

Contact us | Print | Back to top | Help
Copyright © 2014 IUPHAR