TABLE 2.

Pharmacological profile of P2X2R

EC₅₀/IC₅₀ values are micromolar unless otherwise specified.

Compound	Method	EC50/IC50	References
Full agonists
ATP	Current	2–8	Evans et al., 1995; Eickhorst et al., 2002, Zemkova et al., 2004
2-meSATP	Current/Ca2+	1	Evans et al., 1995; Lynch et al., 1999
Ap4A	Current	15	Wildman et al., 1999a
Partial agonists
αβ-meATP	Current	>100	Brake et al., 1994; Evans et al., 1995
βγ-meATP	Current	>300	Evans et al., 1995
ATPγS	Current	10	Evans et al., 1995; Liu et al., 2001
BzATP	Current	6–30	Evans et al., 1995; Lynch et al., 1999
Antagonists
Suramin	Current	10	Brake et al., 1994; Evans et al., 1995
PPADS	Current	1–3	Evans et al., 1995; Lynch et al., 1999
TNP-ATP	Current	2	Virginio et al., 1998b
RB-2	Current	0.5	Liu et al., 2001a
NF279	Current	1	Rettinger et al., 2000
NF770	Current	19 nM	Wolf et al., 2011
NF776	Current	97 nM	Wolf et al., 2011
NF778	Current	140 nM	Wolf et al., 2011
PSB-1011	Current	79 nM	Baqi et al., 2011
PSB-10211	Current	86 nM	Baqi et al., 2011
Modulators
Protons (+)	Current	pKa 7.3	Stoop et al., 1997; Clyne et al., 2002a
Calcium (−)a	Current	5 mM	Evans et al., 1996; Ding and Sachs, 2000
Zinc (+)b,c	Current	30	Brake et al., 1994; Clyne et al., 2002a; Lorca et al., 2005
Cooper (+)c	Current	3	Xiong et al., 1999; Lorca et al., 2005
Cadmium (+)	Current	>100	Lorca et al., 2005
Lanthanum (−)	Current	10	Nakazawa et al., 1997
Gadolinium (−)	Current	1	Nakazawa et al., 1997
Mercury (+)d	Current	10	Lorca et al., 2005; Coddou et al., 2009
H2O2 (+)d	Current	300	Coddou et al., 2009
Myxothiazol (+)d	Current	100 nM	Coddou et al., 2009
Rotenone (+)d	Current	600 nM	Coddou et al., 2009
CO (+)	Current	3	Wilkinson et al., 2009
Progesterone (+)	Current	10	De Roo et al., 2010
DHEA (+)	Current	10	De Roo et al., 2003
PIPse	Current	N.D.	Fujiwara and Kubo, 2006
Ethanol (−)	Current	100 mM	Davies et al., 2002; Popova et al., 2010
Toluene (+)	Current	3 mM	Woodward et al., 2004
PKA (−)	Current		Chow and Wang, 1998
VILIP1 (−)	Current		Chaumont et al., 2008

(+), positive modulator; (−), negative modulator; DHEA, dehydroepiandrosterone; PIPs, phosphoinositides; N.D., not determined; VILIP1, visinin-like protein 1.

^a In addition, induces an increase in receptor desensitization/inactivation, also observed with Ba²⁺, Mn²⁺, and Mg²⁺.

^b Inhibition at human P2X2R (Tittle and Hume, 2008).

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

^d Through the oxidation of the intracellular Cys⁴³⁰.

^e Regulation of receptor desensitization by phosphatidylinositol 3-phosphate and phosphatidylinositol 3,5-bisphosphate.