Table 9.
Binding Affinities of Known ASIC Ligands
| Ligand | Subunit | IC50 |
|---|---|---|
|
| ||
| A-317567 [301] | ASIC1 | 2.0 µM |
| ASIC2 | 29.1 µM | |
| ASIC3 | 9.5 µM | |
| Amiloride [263, 301-302] | ASIC1a | 10 µM |
| ASIC1b | 21 µM | |
| ASIC2a | 0.15 µM | |
| ASIC3 | 37.2 µM | |
| ASIC3 | 63.0 µM | |
| APETx2 (Sea anemone toxin) [303] | ASIC3 | 63.0 nM |
| ASIC1a+3 | 2.0 µM | |
| ASIC1b+3 | 0.9 µM | |
| ASIC2b+3 | 117.0 nM | |
| Acetylsalicylic acid [304] | ASIC3 | 260 µM |
| DAPI [305] | ASIC in hippocampal neurons | 2.8 µM |
| Diclofenac [304] | ASIC3 | 92 µM |
| Diminazene [305] | ASIC in hippocampal neurons | 0.3 µM |
| Flurbiprofen [304] | ASIC1a | 350 µM |
| Gentamycin [306] | ASIC in dorsal root ganglion neurons | 44 µM |
| Hydroxystilbamidine [305] | ASIC in hippocampal neurons | 1.5 µM |
| Ibuprofen [304] | ASIC1a | 350 µM |
| Nafamostat [307] | ASIC depending on the subunit | 2-70 µM |
| Neomycin [306] | ASIC in dorsal root ganglion neurons | 32 µM |
| PcTx-1 (Tarantula toxin, psalmotoxin 1) [308-310] | ASIC1a | 0.9 nM |
| Pentamidine [305] | ASIC in hippocampal neurons | 38 µM |
| Synthalin [305] | ASIC in hippocampal neurons | 29 µM |