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. 2011 Sep;63(3):641–683. doi: 10.1124/pr.110.003129

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.

a

In addition, a sensitization of ATP-evoked currents is observed with calcium.

b

Biphasic effects, suggesting the existence of more than one allosteric site.