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.