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

TABLE 6.

Pharmacological profile of P2X7R

EC50/IC50 values are micromolar unless otherwise specified.

Compound Method EC50/IC50 References
Full agonists
    ATP Current/Ca2+ 2–4 mM Yan et al., 2010; Donnelly-Roberts et al., 2009a; Roger et al., 2008
    BzATP Current/Ca2+ 10 Yan et al., 2010; Donnelly-Roberts et al., 2009a
Partial agonists
    αβ-meATP Current >300 Surprenant et al., 1996
    βγ-meATP Current >300 Surprenant et al., 1996
    2-meSATP Current 200 Surprenant et al., 1996
Antagonists
    Suramin Current >300 Surprenant et al., 1996
    NF279 Ca2+ 3–20 Donnelly-Roberts et al., 2009a; Klapperstück et al., 2000
    PPADS Current 10–45 Surprenant et al., 1996
    PPNDS Ca2+ 1–10 Donnelly-Roberts et al., 2009a
    MRS2159 Calcium 5 Donnelly-Roberts et al., 2009a
    KN-62 Ca2+ 10 Donnelly-Roberts et al., 2009a
    BBG Current 15–250 nM Jiang et al., 2000a
    oATP Current 100–300 Surprenant et al., 1996; Michel et al., 2000; Hibell et al., 2001
    A740003 Calcium 20–700 nM Honore et al., 2006; Donnelly-Roberts et al., 2009a
    A438079 Current/ 0.2–1 Nelson et al., 2006; Donnelly-Roberts et al., 2009a
    A804598 Ca2+ 10 nM Donnelly-Roberts et al., 2009b
    AZ10606120 Ethidium/Ca2+ 10–200 nM Michel et al., 2007
    AZ11645373 Current 5–10 nM Stokes et al., 2006
Modulators
    Protons (−) Current pKa 6.1 Virginio et al., 1997; Acuña-Castillo et al., 2007; Liu et al., 2009
    Calcium (−) Current 3 mM Surprenant et al., 1996; Virginio et al., 1997
    Magnesium (−) Current 500 Virginio et al., 1997; Acuña-Castillo et al., 2007
    Zinc (−) Current 80 Virginio et al., 1997; Acuña-Castillo et al., 2007; Liu et al., 2008a
    Cooper (−) Current 2 Virginio et al., 1997; Acuña-Castillo et al., 2007; Liu et al., 2008a
    PIPs (+) Current N.D. Zhao et al., 2007a,b
    Propofol (+) Current 100 Nakanishi et al., 2007
    Ketamine (+) Current 3 mM Nakanishi et al., 2007
    GW791343 (+)a Ethidium 10 Michel at al., 2008
    Calmodulin (+) Current Roger et al., 2008
    LPC (+) Ca2+ Takenouchi et al., 2007
    Polymyxin B (+) Ca2+ 0.5 μg/ml Ferrari et al., 2006

(+), positive modulator; (−), negative modulator; oATP, oxidized ATP; PIPs, phosphoinositides; N.D., not determined.

a

Positive modulator at rat and negative modulator at human P2X7R (Michel et al., 2008).