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. 2013 Dec 17;170(8):1582–1606. doi: 10.1111/bph.12446
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)