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

GluN2C

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

   GtoImmuPdb view: OFF :     Currently no data for GluN2C in GtoImmuPdb

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, ionotropic, NMDA2C (epsilon 3)
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 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
(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]
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 Units 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 Units 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

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluN2C. Last modified on 01/03/2016. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=458.