TABLE 3.

Pharmacological Profile of P2X3R

EC₅₀/IC₅₀ values are micromolar unless otherwise specified.

Compound	Method	EC50/IC50	References
Full agonists
ATP	Current	1	Lewis et al., 1995; Chen et al., 1995
αβ-meATP	Current	1–2	Lewis et al., 1995; Chen et al., 1995
2-meSATP	Current	0.3	Lewis et al., 1995; Chen et al., 1995; Garcia-Guzman et al., 1997
Ap6A	Current	1.5	Wildman et al., 1999a
Ap5A	Current	1	Wildman et al., 1999a
Ap4A	Current	1	Wildman et al., 1999a
Partial agonists
ATPγS	Current	10	Liu et al., 2001
BzATP	Calcium	N.D.	Jarvis et al., 2001; He et al., 2002
βγ-meATP	Current	>300	Chen et al., 1995
Antagonists
Suramin	Current	3	Lewis et al., 1995
PPADS	Current	1.5	Lewis et al., 1995
TNP-ATP	Current	1 nM	Virginio et al., 1998b
A-317491	Current/Ca2+	20 nM	Jarvis et al., 2002
NF023	Current	8.5	Soto et al., 1999
NF279	Current	2	Rettinger et al., 2000
NF449	Current	3	Braun et al., 2001
RO-85	Calcium	30 nM	Brotherton-Pleiss et al., 2010
Ip4I	Current	1	King et al., 1999
MRS2159	Current	150 nM	Kim et al., 2001
MRS2257	Current	30 nM	Kim et al., 2001
AF-353	Current/Ca2+	10 nM	Gever et al., 2010
RO-4	Calcium	13 nM	Carter et al., 2009
RO-51	Calcium	10 nM	Jahangir et al., 2009
Modulators
Protons (−)	Current	pKa 6.0	Stoop et al., 1997; Gerevich et al., 2007
Calcium (−)	Current	90 mM	Virginio et al., 1998a
Zinc (+) a	Current	10	Wildman et al., 1999b
Cadmium (−)	Current	100	Nakazawa and Ohno, 1997
Ethanol (+)	Current	25 mM	Davies et al., 2005a
Cibracon Blue (+)	Current/Ca2+	1.5	Alexander et al., 1999
Toluene (−)	Current	3 mM	Woodward et al., 2004
Tetramethylpyrazine	Current	1 mM	Gao et al., 2008
Cdk-5 (−)	Current		Nair et al., 2010
Csk (−)	Current		D'Arco et al., 2009

N.D., not determined; (+), positive modulator; (−), negative modulator; Cdk-5, cyclin-dependent kinase 5; Src, C-terminal Src kinase.

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