GluK2 | Ionotropic glutamate receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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Target not currently curated in GtoImmuPdb

Target id: 451

Nomenclature: GluK2

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 1 908 6q16.3-q21 GRIK2 glutamate ionotropic receptor kainate type subunit 2
Mouse 3 1 869 10 B3 Grik2 glutamate receptor, ionotropic, kainate 2 (beta 2)
Rat 3 1 908 20q13 Grik2 glutamate ionotropic receptor kainate type subunit 2
Previous and Unofficial Names
EAA4 | GLUK6 | GluR6 | MRT6 | glutamate receptor 6 | Glurbeta2 | glutamate receptor, ionotropic, kainate 2 | glutamate receptor, ionotropic, kainate 2 (beta 2) | glutamate receptor
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Electron density map of GluK2 desensitized state in complex with 2S,4R-4-methylglutamate
Ligand:  SYM2081
Resolution:  0.0Å
Species:  Rat
References:  2
Natural/Endogenous Ligands
L-glutamic acid

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]kainate Rn Full agonist 8.2 pKd 7
pKd 8.2 (Kd 6.6x10-9 M) [7]
dysiherbaine Rn Full agonist 8.9 pKi 5
pKi 8.9 (Ki 1.2x10-9 M) [5]
kainate Rn Agonist 7.8 – 8.4 pKi 1,7
pKi 7.8 – 8.4 (Ki 1.43x10-8 – 3.7x10-9 M) [1,7]
Description: Measured using kainic acid in rat forebrain homogenate.
SYM2081 Hs Agonist 8.0 pKi 3
pKi 8.0 (Ki 1x10-8 M) [3]
SYM2081 Rn Agonist 7.8 – 8.0 pKi 4,7
pKi 7.8 – 8.0 (Ki 1.7x10-8 – 9.8x10-9 M) [4,7]
Description: Measuring displacement of [3H]kainate binding to recombinant rGluR6 receptors.
domoic acid Hs Full agonist 7.7 pKi 1
pKi 7.7 (Ki 1.83x10-8 M) [1]
Description: Measuring displacement of [3H]Kainate binding by domoate.
kainate Hs Full agonist 7.3 – 7.5 pKi 1,6
pKi 7.3 – 7.5 (Ki 5.3x10-8 – 3.2x10-8 M) [1,6]
Description: Measured using kainic acid.
LY339434 Hs Agonist 4.8 – 4.9 pKi 6
pKi 4.8 – 4.9 (Ki 1.541x10-5 – 1.204x10-5 M) [6]
SYM2081 Rn Full agonist 7.7 pIC50 7
pIC50 7.7 (IC50 1.9x10-8 M) [7]
[3H]SYM2081 Hs Full agonist - -
View species-specific agonist tables
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
2,4-epi-neodysiherbaine Hs Antagonist - -
Allosteric Modulators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
concanavalin A Hs Positive - - - no

Not voltage dependent
Clinically-Relevant Mutations and Pathophysiology
Disease:  Mental retardation, autosomal recessive, 6; MRT6
Synonyms: Autosomal recessive non-syndromic intellectual disability [Orphanet: ORPHA88616]
OMIM: 611092
Orphanet: ORPHA88616


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1. Cantrell BE, Zimmerman DM, Monn JA, Kamboj RK, Hoo KH, Tizzano JP, Pullar IA, Farrell LN, Bleakman D. (1996) Synthesis of a series of aryl kainic acid analogs and evaluation in cells stably expressing the kainate receptor humGluR6. J. Med. Chem., 39 (19): 3617-24. [PMID:8809152]

2. Meyerson JR, Kumar J, Chittori S, Rao P, Pierson J, Bartesaghi A, Mayer ML, Subramaniam S. (2014) Structural mechanism of glutamate receptor activation and desensitization. Nature, 514 (7522): 328-34. [PMID:25119039]

3. Pedregal C, Collado I, Escribano A, Ezquerra J, Domínguez C, Mateo AI, Rubio A, Baker SR, Goldsworthy J, Kamboj RK et al.. (2000) 4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists. J. Med. Chem., 43 (10): 1958-68. [PMID:10821708]

4. Sagot E, Pickering DS, Pu X, Umberti M, Stensbøl TB, Nielsen B, Chapelet M, Bolte J, Gefflaut T, Bunch L. (2008) Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7. J. Med. Chem., 51 (14): 4093-103. [PMID:18578478]

5. Sakai R, Swanson GT, Shimamoto K, Green T, Contractor A, Ghetti A, Tamura-Horikawa Y, Oiwa C, Kamiya H. (2001) Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea. J. Pharmacol. Exp. Ther., 296 (2): 650-8. [PMID:11160654]

6. Small B, Thomas J, Kemp M, Hoo K, Ballyk B, Deverill M, Ogden AM, Rubio A, Pedregal C, Bleakman D. (1998) LY339434, a GluR5 kainate receptor agonist. Neuropharmacology, 37 (10-11): 1261-7. [PMID:9849663]

7. Zhou LM, Gu ZQ, Costa AM, Yamada KA, Mansson PE, Giordano T, Skolnick P, Jones KA. (1997) (2S,4R)-4-methylglutamic acid (SYM 2081): a selective, high-affinity ligand for kainate receptors. J. Pharmacol. Exp. Ther., 280 (1): 422-7. [PMID:8996224]


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