Table 1

Agonist potency at homomeric P2X receptors.

rP2X5rP2X1
EC50nHEC50nH
μM μM
ATP0.44  ± 0.051.4  ±  0.20.10  ± 0.070.8  ±  0.3
2MeSATP0.44  ± 0.151.2  ±  0.10.10  ± 0.030.7  ±  0.2
ATPγS0.29  ± 0.170.7  ±  0.20.59  ± 0.231-a 1.0  ±  0.2
α,β-meATP1.1  ± 0.21-a 1.3  ±  0.63.2  ± 0.21-a 0.8  ±  0.4
BzATP1.3  ± 0.91-a 0.8  ±  0.224.2  ± 0.20.8  ±  0.1
GTP25.1  ± 0.10.9  ±  0.3Inactive
CTP46.2  ± 0.91.1  ±  0.235.1  ± 0.21-a 0.6  ±  0.3
β,γ-meATP11.8  ± 0.21-a 1.4  ±  0.68.7  ± 0.21-a 0.6  ±  0.4
ADP3.6  ± 0.31-a 1.3  ±  1.0Inactive
UTP8.2  ± 0.11-a 1.5  ±  0.761.2  ± 0.31-a 0.4  ±  0.4
ITPInactiveInactive
UDPInactiveInactive
Ap2AInactiveInactive
Ap3A5.4  ± 0.21-a 1.4  ±  0.61.2  ± 0.51-a 1.1  ±  0.3
Ap4A0.25  ± 0.11-a 1.1  ±  0.20.04  ± 0.011-a 1.0  ±  0.3
Ap5A0.69  ± 0.21-a 1.3  ±  0.60.90  ± 0.101-a 0.9  + 0.1
Ap6A4.8  ± 0.21-a 1.5  ±  0.60.60  ± 0.071.0  ±  0.2
PPADS0.20  ± 0.020.6  ±  0.10.12  ± 0.071.5  ±  0.3
TNP-ATP0.45  ± 0.180.6  ±  0.20.001  ± 0.00070.8  ±  0.1
Suramin1.5  ± 0.200.7  ±  0.21.7  ± 0.720.9  ±  0.1
RB-218.3  ± 0.810.9  ±  0.12.3  ± 1.001.1  ±  0.3
Ip5I>300.003  ± 0.00080.9  ±  0.2

EC50 and n H values at pH 7.5.

    • 1-a Partial agonist.