| Nomenclature | AMPA | Kainate |
|---|---|---|
| Ensembl Gene family ID | ENSF00000000118 | ENSF00000000118 |
| Selective agonists | AMPA, (S)-5-fluorowillardiine | ATPA, (S)-4-AHCP, 8-deoxy-neodysiherbaine, (S)-5-iodowillardiine, LY339434 (all selective for receptors containing a GluK1 subunit), (2S,4R)-4-methylglutamate (SYM2081), dysiherbaine, domoic acid (inactive at GluK3), kainate (low potency at GluK3) |
| Selective antagonists | NBQX, ATPO, LY293558, GYKI53655/LY300168 (active isomer GYKI53784/LY303070) (noncompetitive) | UBP302, UBP310, ACET, LY382884, LY466195 (all selective for receptors containing a GluK1 subunit), NS3763 (non-competitive, GluK1 selective), MSVIII-19 (GluK1 selective), 2,4-epi-neodysiherbaine (GluK1 and GluK2 selective) |
| Positive modulators | Pyrrolidinones (piracetam, aniracetam), benzothiadiazides (cyclothiazide, S18986, IDRA-21), benzylpiperidines (CX-516 (BDP-12), CX-546), biarylpropylsulfonamides (LY392098, LY404187 and LY503430) | Concanavalin A (GluK1 and GluK2, not GluK3) |
| Channel blockers | Intracellular polyamines, extracellular argiotoxin, extracellular Joro toxin, (selective for channels lacking GluA2) | Intracellular polyamines (subtype selective; GluK3 >> GluK2) |
| Probes (Kd) | [3H]AMPA, [3H]CNQX | [3H]Kainate, [3H](2S,4R)-4-methylglutamate, [3H]UBP310 (GluK1, 21 nM, GluK3, 0.56 µM, Atlason et al., 2010) |
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