Pharmacological characteristics of adenosine receptor subtypes
| Adenosine receptor | Order of potency for agonists1-a(μM) | Selective agonists1-b | Selective antagonists1-b |
|---|---|---|---|
| A1 | R-PIA (0.001) > NECA (0.006) > IB-MECA (0.054) > CGS 21680 (2.6) | R-PIA, CPA | DPCPX, N-0861 |
| A2A | NECA (0.01) = CGS 21680 (0.015) > IB-MECA (0.056) > R-PIA (0.124) | CGS 21680, APEC | SCH 58261, ZM 241385 |
| A2B | NECA (2) > R-PIA (160) = IB-MECA (201) > CGS 21680 (1600) | None | Enprofylline |
| A3 | IB-MECA (0.001) > NECA (0.113) = R-PIA (0.158) > CGS 21680 (0.584) | IB-MECA, CI-IB-MECA | MRS 1067, MRS 1097 L-249313, L-268605 |
↵1-a Data shown for rat A1, A2A, and A3 receptors are Ki values based on radioligand binding, from van Galen et al. (1994) andGallo-Rodriguez et al. (1994). Data shown for A2B receptors are EC50 values for cAMP accumulation in human erythroleukemia cells from Feoktistov and Biaggioni (1993) andFeoktistov and Biaggioni (1997a).
↵1-b Data are derived from Feoktistov and Biaggioni (1995),Palmer and Stiles (1995), Jacobson et al. (1996), and Jacobson (1996).