GluN2C | Ionotropic glutamate receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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GluN2C

Target not currently curated in GtoImmuPdb

Target id: 458

Nomenclature: GluN2C

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 1233 17q25 GRIN2C glutamate ionotropic receptor NMDA type subunit 2C
Mouse 3 1 1239 11 E2 Grin2c glutamate receptor
Rat 3 1 1250 10q32.2 Grin2c glutamate ionotropic receptor NMDA type subunit 2C
Previous and Unofficial Names
NMDAR2C | glutamate [NMDA] receptor subunit epsilon-3 | GluRepsilon3 | glutamate receptor, ionotropic, NMDA2C (epsilon 3) | glutamate receptor
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
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 Parameter 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
(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 Parameter 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]
UBP141 Hs Antagonist - - 3
[Binds to: glutamate site] GluN2D ≥ GluN2C > GluN2A ≥ GluN2B [3]
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Affinity Parameter Concentration range (M) Voltage-dependent (mV) Reference
phencyclidine Hs - no 7.1 pIC50 - no 2
pIC50 7.1 (IC50 7.7x10-8 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
dextrorphan Hs - no 6.9 pIC50 - no 2
pIC50 6.9 (IC50 1.14x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
dextromethorphan Hs - no 6.3 pIC50 - no 2
pIC50 6.3 (IC50 4.66x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
levorphanol Hs - no 6.2 pIC50 - no 2
pIC50 6.2 (IC50 6.01x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
ketamine Hs - no 6.2 pIC50 - no 2
pIC50 6.2 (IC50 6.6x10-7 M) [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
amantidine Hs - no 4.7 pIC50 - no 2
pIC50 4.7 (IC50 2.25x10-5 M) GluN2C = GluN2D ≥ GluN2B ≥ GluN2A [2]
Not voltage dependent
Description: Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9
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
N1-dansyl-spermine Hs - no - - - no
GluN2A = GluN2B >> GluN2C = GluN2D
Not voltage dependent
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Concentration range (M) Voltage-dependent (mV) Reference
DQP-1105 Rn Negative 8.1 pIC50 - no 1
pIC50 8.1 (IC50 7x10-9 M) [1]
Not voltage dependent
Description: Measured using recombinant GluN1-1a NMDA subunits co-expressed with GluN2C subunits.

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. Dravid SM, Erreger K, Yuan H, Nicholson K, Le P, Lyuboslavsky P, Almonte A, Murray E, Mosely C, Barber J et al.. (2007) Subunit-specific mechanisms and proton sensitivity of NMDA receptor channel block. J. Physiol. (Lond.), 581 (Pt 1): 107-28. [PMID:17303642]

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]

Contributors

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How to cite this page

Bernhard Bettler, Graham L. Collingridge, Ray Dingledine, Stephen F. Heinemann, Michael Hollmann, Juan Lerma, David Lodge, Mark Mayer, Masayoshi Mishina, Christophe Mulle, Shigetada Nakanishi, Richard Olsen, Stephane Peineau, John A. Peters, Peter Seeburg, Michael Spedding, Jeffrey C. Watkins, Robert J. Wenthold.
Ionotropic glutamate receptors: GluN2C. Last modified on 01/03/2016. Accessed on 26/03/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=458.