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 | glutamate receptor, ionotropic, NMDA2A (epsilon 1) | glutamate receptor
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
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 22/05/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=456.