Table 1.
P2X4 modulators and antagonists.
| Compound | Nature | Potency at P2X4 IC50 μM (species) | Selectivity | Reference |
|---|---|---|---|---|
| 5-BDBD | Competitive | 1.6 (Human) | Not reported | Balazs et al., 2013; Abdelrahman et al., 2016 |
| PSB-12054 | Allosteric | 0.189 (Human) | 30-fold (P2X1) | Hernandez-Olmos et al., 2012 |
| 2.10 (Rat) | 50-fold (P2X2, 3, 7) | |||
| 1.77 (Mouse) | ||||
| PSB-12062 | Allosteric | 1.38 (Human) | 35-fold (P2X1-3, 7) | Hernandez-Olmos et al., 2012 |
| 0.928 (Rat) | ||||
| 1.76 (Mouse) | ||||
| BX-430 | Non-competitive allosteric | 0.54 (Human) | 10-fold (P2X1-3, 5) | Ase et al., 2015 |
| 100-fold (P2X7) | ||||
| 1.89 (Zebrafish) | ||||
| Carbamazepine derivative | Negative allosteric modulator | 3.44 (Human) | 2-fold (P2X1, 3) | Tian et al., 2014 |
| 30-fold (P2X2, 7) | ||||
| 54.6 (Rat) | ||||
| 14.9 (Mouse) | ||||
| NP-1815-PX | Not reported | 0.26 (Human) | Not reported | Matsumura et al., 2016 |
| Ivermectin | Positive allosteric modulator | 0.25 (Human) | Acts on human P2X7 | Priel and Silberberg, 2004; Nörenberg et al., 2012 |
| Cibacron blue | Potentiator | Not determined | Not reported | Miller et al., 1998 |