Nomenclature |
GluK1 |
GluK2 |
GluK3 |
GluK4 |
GluK5 |
HGNC, UniProt |
GRIK1, P39086
|
GRIK2, Q13002
|
GRIK3, Q13003
|
GRIK4, Q16099
|
GRIK5, Q16478
|
Agonists (EC50) |
8-deoxy-neodysiherbaine (Full agonist), ATPA (Full agonist), domoic acid (Full agonist), dysiherbaine (Full agonist), (S)-4-AHCP (Full agonist), (S)-5-iodowillardiine, kainate (Full agonist), LY339434 (Full agonist), SYM2081 (Full agonist) |
domoic acid (Full agonist), dysiherbaine (Full agonist), kainate (Full agonist), SYM2081 (Full agonist) |
dysiherbaine (Full agonist), kainate (Full agonist, low potency), SYM2081 (Full agonist) |
domoic acid (Full agonist), dysiherbaine (Full agonist), kainate (Full agonist), SYM2081 (Full agonist) |
domoic acid (Full agonist), dysiherbaine (Full agonist), kainate (Full agonist), SYM2081 (Full agonist) |
Selective antagonists (IC50) |
2,4-epi-neodysiherbaine, ACET, LY382884, LY466195, MSVIII-19, NS3763 (non-competitive), UBP302, UBP310 |
2,4-epi-neodysiherbaine |
– |
– |
– |
Allosteric Regulators |
concanavalin A (Positive) |
concanavalin A (Positive) |
– |
– |
– |
Radioligands (Kd) |
[3H](2S,4R)-4-methylglutamate, [3H]kainate, [3H]UBP310 (2.1x10-8 M) 138
|
[3H](2S,4R)-4-methylglutamate, [3H]kainate |
[3H](2S,4R)-4-methylglutamate, [3H]kainate, [3H]UBP310 (5.6x10-7 M) 138
|
[3H](2S,4R)-4-methylglutamate, [3H]kainate |
[3H](2S,4R)-4-methylglutamate, [3H]kainate |
Comment |
– |
Intracellular polyamines are subtype selective channel blockers (GluK3 >> GluK2) |
domoic acid and concanavalin A are inactive at the GluK3 subunit. Intracellular polyamines are subtype selective channel blockers (GluK3 >> GluK2) |
– |
– |