GluK1 | Ionotropic glutamate receptors | IUPHAR/BPS Guide to PHARMACOLOGY

GluK1

Target id: 450

Nomenclature: GluK1

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 GluK1 in GtoImmuPdb

Gene and Protein Information
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 905 21q22.11 GRIK1 glutamate ionotropic receptor kainate type subunit 1
Mouse 3 1 905 16 C3.3 Grik1 glutamate receptor, ionotropic, kainate 1
Rat 3 1 920 11q11 Grik1 glutamate ionotropic receptor kainate type subunit 1
Previous and Unofficial Names
EAA3 | GluR5 | glutamate receptor 5 | GluK5 | Glurbeta1 | glutamate receptor
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
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
SYM2081 Rn Agonist 9.2 pKi 3
pKi 9.2 (Ki 6.63x10-10 M) [3]
dysiherbaine Rn Full agonist 9.1 pKi 4
pKi 9.1 (Ki 7.4x10-10 M) [4]
SYM2081 Hs Full agonist 8.5 pKi 2
pKi 8.5 (Ki 3x10-9 M) [2]
LY339434 Hs Agonist 7.8 – 7.9 pKi 5
pKi 7.8 – 7.9 (Ki 1.5x10-8 – 1.3x10-8 M) [5]
kainate Hs Full agonist 6.8 pKi 5
pKi 6.8 (Ki 1.77x10-7 M) [5]
(S)-4-AHCP Hs Full agonist - -
(S)-5-iodowillardiine Hs Agonist - -
[3H]SYM2081 Hs Full agonist - -
[3H]kainate Hs Full agonist - -
8-deoxy-neodysiherbaine Hs Full agonist - -
ATPA Hs Full agonist - -
domoic acid Hs Full agonist - -
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]UBP310 Hs Antagonist 7.7 pKd 1
pKd 7.7 (Kd 2.1x10-8 M) [1]
2,4-epi-neodysiherbaine Hs Antagonist - -
ACET Hs Antagonist - -
LY382884 Hs Antagonist - -
LY466195 Hs Antagonist - -
MSVIII-19 Hs Antagonist - -
NS3763 Hs Antagonist - -
non-competitive
UBP302 Hs Antagonist - -
UBP310 Hs Antagonist - -
Allosteric Modulators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
concanavalin A Hs Positive - - - no

Not voltage dependent

References

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1. Atlason PT, Scholefield CL, Eaves RJ, Mayo-Martin MB, Jane DE, Molnár E. (2010) Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310. Mol. Pharmacol., 78 (6): 1036-45. [PMID:20837679]

2. 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]

3. 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]

4. 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]

5. 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]

Contributors

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How to cite this page

John A. Peters, Stephane Peineau, Graham L Collingridge, Robert J. Wenthold.
Ionotropic glutamate receptors: GluK1. Last modified on 20/10/2015. Accessed on 24/09/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=450.