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
GenitoUrinary Development Molecular Anatomy Project
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. Neuropharmacology37 (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 27/04/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=450.