GluN2A

Target id: 456

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.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GluN2A in GtoImmuPdb

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 1464 16p13.2 GRIN2A glutamate ionotropic receptor NMDA type subunit 2A
Mouse 3 1 1464 16 A1 Grin2a glutamate receptor, ionotropic, NMDA2A (epsilon 1)
Rat 3 1 1464 10q11 Grin2a glutamate ionotropic receptor NMDA type subunit 2A
Previous and Unofficial Names
NMDAR2A | GluRepsilon1 | NMDA-R2A | glutamate receptor, ionotropic, N-methyl D-aspartate 2A
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
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
glycine Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
L-aspartic acid Hs Agonist - -
[Binds to: glutamate site] GluN2D = GluN2B > GluN2C = GluN2A
(+)-HA966 Hs Partial agonist - -
[Binds to: glycine site] GluN2B > GluN2A
(RS)-(tetrazol-5-yl)glycine Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
[3H]glycine Hs Agonist - -
[Binds to: glycine site]
D-serine Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
homoquinolinic acid Hs Full agonist - -
[Binds to: glutamate site] GluN2B ≥ GluN2A ≥ GluN2D > GluN2C; partial agonist at GluN2A and GluN2C
NMDA Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C > GluN2B > GluN2A
D-aspartic acid Hs Agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
5,7-dichlorokynurenic acid Hs Antagonist - -
[Binds to: glycine site]
[3H]CGP39653 Hs Antagonist - -
[Binds to: glutamate 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]
[3H]L689560 Hs Antagonist - -
[Binds to: glycine site]
[3H]MDL105519 Hs Antagonist - -
[Binds to: glycine site]
CGP37849 Hs Antagonist - -
[Binds to: glutamate site]
selfotel Hs Antagonist - -
[Binds to: glutamate site]
conantokin-G Hs Antagonist - -
[Binds to: glutamate site] GluN2B > GluN2D = GluN2C = GluN2A
d-AP5 Hs Antagonist - -
[Binds to: glutamate site]
d-CCPene Hs Antagonist - -
[Binds to: glutamate site] GluN2A = GluN2B > GluN2C = GluN2D
GV196771A Hs Antagonist - -
[Binds to: glycine site]
L689560 Hs Antagonist - -
[Binds to: glycine site]
L701324 Hs Antagonist - -
[Binds to: glycine site]
LY233053 Hs Antagonist - -
[Binds to: glutamate site]
NVP-AAM077 Hs Antagonist - - 1-3,6
[Binds to: glutamate site] GluN2A > GluN2B (human), but weakly selective for rat GluN2A versus GluN2B [1-3,6]
UBP141 Hs Antagonist - - 5
[Binds to: glutamate site] GluN2D ≥ GluN2C > GluN2A ≥ GluN2B [5]
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
Mg2+ Hs - no - - - no
GluN2A = GluN2B > GluN2C = GluN2D
Not voltage dependent
dizocilpine Hs - no - - - no

Not voltage dependent
[3H]dizocilpine Hs - no - - - no
[Binds to: cation channel]
Not voltage dependent
amantidine Hs - no - - - no
GluN2C = GluN2D ≥ GluN2B ≥ GluN2A
Not voltage dependent
ketamine Hs - no - - - no

Not voltage dependent
N1-dansyl-spermine Hs - no - - - no
GluN2A = GluN2B >> GluN2C = GluN2D
Not voltage dependent
phencyclidine Hs - no - - - no

Not voltage dependent
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
TCN-201 Hs Negative 7.0 pIC50 - no 4
pIC50 7.0 (IC50 1x10-7 M) [4]
Not voltage dependent
Description: Inhibition of glycine-induced (1µM) NMDA receptor responses measured in Xenopus oocytes co-expressing hGluN1 and hGluN2A NMDA receptor subunits
Clinically-Relevant Mutations and Pathophysiology
Disease:  Epilepsy, focal, with speech disorder and with or without mental retardation; FESD
Synonyms: Early-onset epileptic encephalopathy and intellectual disability due to GRIN2A mutation [Orphanet: ORPHA289266]
OMIM: 245570
Orphanet: ORPHA289266
Disease:  Epileptic encephalopathy with continuous spike-and-wave during sleep
OMIM: 245570
Orphanet: ORPHA725
Disease:  Landau-Kleffner syndrome
Disease Ontology: DOID:2538
OMIM: 245570
Orphanet: ORPHA98818
Disease:  Rolandic epilepsy
Synonyms: Benign familial epilepsy of childhood with rolandic spikes [Orphanet: ORPHA1945]
OMIM: 245570
Orphanet: ORPHA1945
Disease:  Rolandic epilepsy - speech dyspraxia
OMIM: 245570
Orphanet: ORPHA163721

References

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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. Hansen KB, Ogden KK, Traynelis SF. (2012) Subunit-selective allosteric inhibition of glycine binding to NMDA receptors. J. Neurosci.32 (18): 6197-208. [PMID:22553026]

5. 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]

6. 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]

Contributors

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How to cite this page

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluN2A. Last modified on 13/05/2015. Accessed on 20/11/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=456.