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 GluR5 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 GluR5-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 GLUK5
5032 Talampanel
Non-competitive AMPA/kainate antagonist
3620 Topiramate
GluR5 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 GluR5-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
GLUK5 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 GluR6 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 GluR5-7 and KA1-2 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

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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