GluN2D

Target id: 459

Nomenclature: GluN2D

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

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 1336 19q13.1 GRIN2D glutamate receptor, ionotropic, N-methyl D-aspartate 2D
Mouse 3 1 1323 7 B4 Grin2d glutamate receptor, ionotropic, NMDA2D (epsilon 4)
Rat 3 1 1323 1q22 Grin2d glutamate receptor, ionotropic, N-methyl D-aspartate 2D
Previous and Unofficial Names
EB11
NMDAR2D
GluRepsilon4
NR2D
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
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]
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 - - 3
[Binds to: glutamate site] GluN2D ≥ GluN2C > GluN2A ≥ GluN2B [3]
LY233053 Hs Antagonist - -
[Binds to: glutamate site]
selfotel Hs Antagonist - -
[Binds to: glutamate site]
CGP37849 Hs Antagonist - -
[Binds to: glutamate site]
L701324 Hs Antagonist - -
[Binds to: glycine 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]
[3H]CGP61594 Hs Antagonist - -
[Binds to: glycine site] [3H]CGP61594 is a photoaffinity ligand
GV196771A Hs Antagonist - -
[Binds to: glycine site]
[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
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]dizocilpine 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
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
DQP-1105 Rn Negative 5.57 pIC50 - no 1
pIC50 5.57 (IC50 2.7x10-6 M) [1]
Not voltage dependent
Description: Measured using recombinant GluN1-1a NMDA subunits co-expressed with GluN2D subunits.
QNZ 46 Rn Negative 5.41 – 5.49 pIC50 - no 2
pIC50 5.41 – 5.49 (IC50 3.9x10-6 – 3.2x10-6 M) [2]
Not voltage dependent
Description: Measured using co-expression of recombinant rGluN1 and rGluN2D. IC50 variable between expression cell lines.

References

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1. Acker TM, Yuan H, Hansen KB, Vance KM, Ogden KK, Jensen HS, Burger PB, Mullasseril P, Snyder JP, Liotta DC et al.. (2011) Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators. Mol. Pharmacol.80 (5): 782-95. [PMID:21807990]

2. Hansen KB, Traynelis SF. (2011) Structural and mechanistic determinants of a novel site for noncompetitive inhibition of GluN2D-containing NMDA receptors. J. Neurosci.31 (10): 3650-61. [PMID:21389220]

3. 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]

How to cite this page

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluN2D. Last modified on 31/10/2014. Accessed on 29/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=459.