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.