TABLE 5.
Pharmacological profile of P2X5R
EC50/IC50 values are micromolar unless otherwise specified.
| Compound | Method | EC50/IC50 | References |
|---|---|---|---|
| Full agonists | |||
| ATP | Current | 0.5–4 | Wildman et al., 2002; Bo et al., 2003 |
| 2-meSATP | Current | 0.5 | Wildman et al., 2002 |
| ATPγS | Current | 0.5 | Wildman et al., 2002 |
| Partial agonists | |||
| αβ-meATP | Current | 1–12 | Wildman et al., 2002; Kotnis et al., 2010 |
| βγ-meATP | Current | 10 | Wildman et al., 2002 |
| BzATP | Current | 1–6 | Wildman et al., 2002; Bo et al., 2003 |
| Ap3A | Current | 5 | Wildman et al., 2002 |
| Ap4A | Current | 0.3 | Wildman et al., 2002 |
| Ap5A | Current | 0.7 | Wildman et al., 2002 |
| Ap6A | Current | 5 | Wildman et al., 2002 |
| Antagonists | |||
| Suramin | Current | 2–3 | Wildman et al., 2002; Bo et al., 2003 |
| PPADS | Current | 200–600 nM | Wildman et al., 2002; Bo et al., 2003; Kotnis et al., 2010 |
| TNP-ATP | Current | 600–700 nM | Wildman et al., 2002; Kotnis et al., 2010 |
| BBG | Current | 0.5 | Bo et al., 2003 |
| Modulators | |||
| Protons (−) | Current | Wildman et al., 2002 | |
| Calcium (−)a | Current | 10 mM | Wildman et al., 2002 |
| Zinc (+)b | Current | 10 | Wildman et al., 2002 |
(+), positive modulator; (−), negative modulator.
In addition, a sensitization of ATP-evoked currents is observed with calcium.
Biphasic effects, suggesting the existence of more than one allosteric site.