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GluN2A

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Target not currently curated in GtoImmuPdb

Target id: 456

Nomenclature: GluN2A

Family: Ionotropic glutamate receptors

Gene and Protein Information Click here for help
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 Click here for help
NMDAR2A | GluRepsilon1 | NMDA-R2A | glutamate receptor, ionotropic, N-methyl D-aspartate 2A | glutamate receptor, ionotropic, NMDA2A (epsilon 1) | glutamate receptor
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
D-aspartic acid
D-serine
glycine
L-aspartic acid
L-glutamic acid

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
glycine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
L-aspartic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glutamate site] GluN2D = GluN2B > GluN2C = GluN2A
(+)-HA966 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist - -
[Binds to: glycine site] GluN2B > GluN2A
(RS)-(tetrazol-5-yl)glycine Small molecule or natural product Click here for species-specific activity table Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C = GluN2B > GluN2A
[3H]glycine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Agonist - -
[Binds to: glycine site]
D-serine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist - -
[Binds to: glycine site] GluN2D > GluN2C > GluN2B > GluN2A
homoquinolinic acid Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
[Binds to: glutamate site] GluN2B ≥ GluN2A ≥ GluN2D > GluN2C; partial agonist at GluN2A and GluN2C
NMDA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
[Binds to: glutamate site] GluN2D > GluN2C > GluN2B > GluN2A
D-aspartic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure 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 Value Parameter Reference
5,7-dichlorokynurenic acid Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
[Binds to: glycine site]
[3H]CGP39653 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glutamate site]
[3H]CGP61594 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glycine site] [3H]CGP61594 is a photoaffinity ligand
[3H]CGS19755 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glutamate site]
[3H]CPP Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glutamate site]
[3H]L689560 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glycine site]
[3H]MDL105519 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist - -
[Binds to: glycine site]
CGP37849 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
selfotel Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
conantokin-G Peptide Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site] GluN2B > GluN2D = GluN2C = GluN2A
d-AP5 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
d-CCPene Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site] GluN2A = GluN2B > GluN2C = GluN2D
GV196771A Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glycine site]
L689560 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glycine site]
L701324 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glycine site]
LY233053 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
[Binds to: glutamate site]
NVP-AAM077 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - - 1-3,6
[Binds to: glutamate site] GluN2A > GluN2B (human), but weakly selective for rat GluN2A versus GluN2B [1-3,6]
UBP141 Small molecule or natural product Click here for species-specific activity table 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 Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
Mg2+ Click here for species-specific activity table Hs - no - - - no
GluN2A = GluN2B > GluN2C = GluN2D
Not voltage dependent
dizocilpine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - no - - - no

Not voltage dependent
[3H]dizocilpine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs - no - - - no
[Binds to: cation channel]
Not voltage dependent
amantadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs - no - - - no
GluN2C = GluN2D ≥ GluN2B ≥ GluN2A
Not voltage dependent
ketamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs - no - - - no

Not voltage dependent
N1-dansyl-spermine Small molecule or natural product Click here for species-specific activity table Hs - no - - - no
GluN2A = GluN2B >> GluN2C = GluN2D
Not voltage dependent
phencyclidine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
TCN-201 Small molecule or natural product Primary target of this compound Ligand has a PDB structure 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 Click here for help
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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