TABLE 4.

Pharmacological profile of P2X4R

EC₅₀/IC₅₀ values are micromolar unless otherwise specified.

Compound	Method	EC50/IC50	References
Full agonists
ATP	Current	1–10	Buell et al., 1996; Soto et al., 1996; Jones et al., 2000
BzATP	Calcium	3	He et al., 2003a
Partial agonists
2-meSATP	Current	10–100	Buell et al., 1996; Soto et al., 1996; Jones et al., 2000
αβ-meATP	Current	4–300	Buell et al., 1996; Soto et al., 1996; Jones et al., 2000
βγ-meATP	Current	>300	Soto et al., 1996
CTP	Current	200	Soto et al., 1996
Ap4P	Current	2–10	Wildman et al., 1999a; Jones et al., 2000
Antagonists
Suramin	Current	>300	Buell et al., 1996; Soto et al., 1996
PPADS	Current	>300	Buell et al., 1996; Soto et al., 1996
TNP-ATP	Current	15	Virginio et al., 1998b
5-BDBD	Current	0.5	Donnelly-Roberts et al., 2008
NF023	Current	>100	Soto et al., 1999
BBG	Current	3–100	Jiang et al., 2000a
Paroxetine	Current/Ca2+	2	Nagata et al., 2009
Modulators
Protons (−)	Current	pKa 7.0c	Stoop et al., 1997; Clarke et al., 2000; Yan et al., 2005
Calciuma	Current	1 mM	Khakh et al., 1999a
Zinc (+)b	Current	5	Soto et al., 1996; Xiong et al., 1999; Acuña-Castillo et al., 2000; Coddou et al., 2007
Cooper (−)	Current	10	Acuña-Castillo et al., 2000; Coddou et al., 2003; Coddou et al., 2007
Cadmium (+)b	Current	20	Acuña-Castillo et al., 2000; Coddou et al., 2005
Mercury (−)	Current	10	Coddou et al., 2005; Coddou et al., 2009
H2O2 (−)	Current	300	Coddou et al., 2009
CO (−)	Current	N.D.	Wilkinson et al., 2009
IVM (+)	Current	3	Khakh et al., 1999b; Priel and Silberberg, 2004; Jelínkova et al., 2006; Silberberg et al., 2007
Alfaxalone (+)	Current	0.4 nM	Codocedo et al., 2009
ALP (+)	Current	0.3 nM	Codocedo et al., 2009
THDOC (+)	Current	0.1 nM	Codocedo et al., 2009
PIPs (+)	Current	N.D.	Bernier et al., 2008b
Ethanol (−)	Current	60 mM	Xiong et al., 2000; Davies et al., 2002;
Cibacron blue (+)	Current	3	Miller et al., 1998
Propofol (+)	Current	50	Tomioka et al., 2000
Toluene (+)	Current	1 mM	Woodward et al., 2004
PKA (+)	Current/Ca2+		Brown and Yule, 2010

(+), positive modulator; (−), negative modulator; N.D., not determined; ALP, allopregnanolone; THDOC, 3α,21-dihydroxy-5α-pregnan-20-one; PIPs, phosphoinositides; 5-BDBD, 5-(3-bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one.

^a In the absence of calcium, a secondary current is developed in P2X4Rs.

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