Table 8a

Antagonist selectivities at cloned P2 receptors

ReceptorSuraminPPADSP5PRB2NF023References8-g
P2X1 IC501–5IC50 1IC5010–20N.D.N.D.1,2
P2X2 IC50 1–5IC50 2IC5010–20YesN.D.1,2
P2X3 IC503IC50 1IC50 10N.D.N.D.1
P2X4 rat InactiveInactiveInactiveInactive8-a N.D.1,3–6
(>500 μM)(>100 μM)(>100 μM)(>50 μM)
IC50 46–508-b
IC50 120–1288-c
P2X4 human IC50 178IC5027.5IC50 388-b
IC50398-c
P2X5 IC50 4IC503N.D.N.D.N.D.1
P2X6 InactiveInactiveN.D.N.D.N.D.1
P2X7-human IC50 4IC504.2N.D.N.D.N.D.7,8
P2X7-rat IC504.1IC50 4.3
P2Y1 pA25.4–6pA2 6N.D.N.D.N.D.9–11
P2Y2 pA24.3InactiveN.D.N.D.N.D.10
p2y3pA25N.D.N.D.N.D.N.D.12
P2Y4-human InactiveIC5015/inactiveN.D.Yes8-d N.D.14,15
P2Y4-rat WeakInactiveN.D.IC5021N.D.16
P2Y6 Slight8-e Slight8-f N.D.IC5031N.D.15,17
P2Y11 N.D.N.D.N.D.N.D.N.D.18
  • IC50 and pA2 values are μM; N.D., not determined.

  • 8-a RB2.

  • 8-b Basilen blue (isomer of RB2).

  • 8-c Cibacron blue (isomer of RB2).

  • 8-d 33% inhibition of the UTP response.

  • 8-e Less potent than RB2 and PPADS.

  • 8-f Less potent than RB2.

  • 8-g References: 1 Collo et al., 1996; 2 Evanset al., 1995; 3 Bo et al., 1995; 4 Soto et al., 1996a; 5 Buell et al., 1996b; 6 Garcia-Guzmanet al., 1997a; 7 Surprenant et al., 1996; 8Rassendren et al., 1997; 9 Brown et al., 1995; 10Charlton et al., 1996a; 11 Schachter et al., 1996; 12 Webb et al., 1996a; 13 Charlton et al., 1996b; 14 Communi et al., 1996a; 15 Chang et al., 1995; 16 Bogdanov et al., 1998; 17 Robaye et al., 1997; 18 Communi et al., 1997.