GluN2B

Target id: 457

Nomenclature: GluN2B

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 1484 12p12 GRIN2B glutamate receptor, ionotropic, N-methyl D-aspartate 2B
Mouse 3 1 1482 6 G1 Grin2b glutamate receptor, ionotropic, NMDA2B (epsilon 2)
Rat 3 1 1482 4q43 Grin2b glutamate receptor, ionotropic, N-methyl D-aspartate 2B
Previous and Unofficial Names
NMDAR2B
GluRepsilon2
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
Orphanet Gene
PharmGKB Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of GluN1a/GluN2B NMDA Receptor Ion Channel
PDB Id:  4PE5
Resolution:  3.96Å
Species:  Rat
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of amino terminal domains of the NMDA receptor subunit GluN1 and GluN2B in complex with ifenprodil
PDB Id:  3QEL
Ligand:  ifenprodil
Resolution:  2.6Å
Species:  Rat
References:  6
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]
(+)-HA966 Hs Partial agonist - -
[Binds to: glycine site] GluN2B > GluN2A
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 - - 7
[Binds to: glutamate site] GluN2D ≥ GluN2C > GluN2A ≥ GluN2B [7]
LY233053 Hs Antagonist - -
[Binds to: glutamate site]
selfotel Hs Antagonist - -
[Binds to: glutamate site]
NVP-AAM077 Hs Antagonist - - 2-4,8
[Binds to: glutamate site] GluN2A > GluN2B (human), but weakly selective for rat GluN2A versus GluN2B [2-4,8]
L701324 Hs Antagonist - -
[Binds to: glycine site]
CGP37849 Hs Antagonist - -
[Binds to: glutamate 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] 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 6.95 pIC50 - no 1
pIC50 6.95 (IC50 1.13x10-7 M) [1]
Not voltage dependent
Description: Measured using recombinant GluN1-1a NMDA subunits co-expressed with GluN2C subunits.
Clinically-Relevant Mutations and Pathophysiology
Disease:  Autosomal dominant nonsyndromic intellectual deficit 6
OMIM:  613970
Orphanet:  178469

References

Show »

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. 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]

3. 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]

4. 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]

5. Karakas E, Furukawa H. (2014) Crystal structure of a heterotetrameric NMDA receptor ion channel. Science344 (6187): 992-7. [PMID:24876489]

6. Karakas E, Simorowski N, Furukawa H. (2011) Subunit arrangement and phenylethanolamine binding in GluN1/GluN2B NMDA receptors. Nature475 (7355): 249-53. [PMID:21677647]

7. 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]

8. 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]

How to cite this page

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluN2B. Last modified on 31/10/2014. Accessed on 22/12/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=457.