Kainate Receptors

Kainate receptors are members of the ionotropic class of glutamate receptors, which also includes NMDA and AMPA receptors. Kainate receptors have been identified both pre- and post-synaptically. They contribute to excitatory postsynaptic currents in many regions of the CNS.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1107 ATPA
Selective, potent GluK1 agonist
0269 Domoic acid
Potent, selective kainate agonist
0307 (S)-(-)-5-Iodowillardiine
Highly potent, subtype-selective kainate agonist
0222 Kainic acid
Potent excitant and neurotoxin
2225 MNI caged kainic acid
Caged kainic acid
0903 SYM 2081
Highly selective kainate agonist

Antagonists

Cat No Product Name / Activity
2728 ACET
Potent antagonist of GluK1-containing kainate receptors
0190 CNQX
Potent AMPA/kainate antagonist
1045 CNQX disodium salt
Potent AMPA/kainate antagonist. More water soluble form of Cat. No. 0190
0189 DNQX
Selective non-NMDA antagonist
2312 DNQX disodium salt
Selective non-NMDA antagonist. Water-soluble salt of DNQX (Cat. No. 0189)
0845 Evans Blue tetrasodium salt
AMPA/kainate antagonist
2555 GYKI 53655 hydrochloride
Kainate receptor antagonist; blocks GluK3 receptors
2187 NS 3763
Selective non-competitive kainate antagonist; selective for GluK1
5032 Talampanel
Non-competitive AMPA/kainate antagonist
3620 Topiramate
GluK1 antagonist; inhibits carbonic anhydrase (CA) II and IV
1765 UBP 282
AMPA/kainate antagonist; distinguishes between motoneuron and dorsal root kainate receptors
2078 UBP 296
Selective, potent kainate antagonist; selective for GluK1-containing receptors
1766 UBP 301
Kainate receptor antagonist
2079 UBP 302
Potent and selective kainate antagonist; active enantiomer of UBP 296 (Cat. No. 2078)
3621 UBP 310
GluK1 antagonist
2345 ZK 200775
Competitive AMPA/kainate antagonist

Ligand Sets

Cat No Product Name / Activity
1824 Kainate Receptor Tocriset™
Selection of 5 kainate receptor ligands (Cat. Nos. 0222, 1107, 0903, 1045 and 1454)

Other

Cat No Product Name / Activity
1777 Arctigenin
Binds to kainate receptors; neuroprotective. Also inhibits IκBα phosphorylation and MEK1
2207 PDZ1 Domain inhibitor peptide
Disrupts interaction between GluK2 and PSD-95 PDZ1 domain

Kainate receptors are members of the ionotropic class of glutamate receptors, which also includes NMDA and AMPA receptors. Kainate receptors have been identified both pre- and post-synaptically. The receptors contribute to excitatory postsynaptic currents in many regions of the CNS and play a role in short- and long-term synaptic plasticity. Kainate receptors consist of GluK1-5 subunits. Each subunit has an extracellular N-terminus, a cytoplasmic C-terminus, three membrane-spanning segments and a p-loop that dips into the membrane from the cytoplasmic face to form the pore.

External sources of pharmacological information for Kainate Receptors :

Literature for Kainate Receptors

Tocris offers the following scientific literature for Kainate Receptors to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Kainate Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
GluK1 (formerly GluR5) Human GRIK1 NM_175611 P39086
Mouse Grik1 NM_146072 Q60934
Rat Grik1 NM_017241 P22756
GluK2 (formerly GluR6) Human GRIK2 NM_175768 Q13002
Mouse Grik2 NM_010349 P39087
Rat Grik2 NM_019309 P42260
GluK3 (formerly GluR7) Human GRIK3 NM_000831 Q13003
Mouse Grik3 NM_001081097 NP_001074566
Rat Grik3 NM_181373 P42264
GluK4 (formerly KA-1) Human GRIK4 NM_014619 Q16099
Mouse Grik4 NM_175481 Q8BMF5
Rat grik4 NM_012572 Q01812
GluK5 (formerly KA-2) Human GRIK5 NM_002088 Q16478
Mouse Grik5 NM_008168 Q61626
Rat Grik5 NM_031508 Q63273