Affinities and relative selectivities of the adenosine receptor agonists and antagonists used in this study for the human A1-, A2A-, A2B-, and A3-receptor subtypes
| Ki | Selectivity (Fold) | Reference(s) | ||||
|---|---|---|---|---|---|---|
| A1 | A2A | A2B | A3 | |||
| nM | ||||||
| Agonists | ||||||
| (±)5′-Cl-5′-deoxy-ENBA | 0.5 | 1340 | 2740 | 1290 | A1 (2418–5480) | Franchetti et al., 2009 |
| CGS 21680 | 289 | 27 | 361,000 | 67 | A2A (2–13,370) | Klotz et al., 1998 |
| Bay 60-6583 | >10,000 | >10,000 | 3.0 | >10,000 | A2B (>3333) | Kuno et al., 2007 |
| HEMADO | 327 | 1230 | >30000 | 1.1 | A3 (297 to >27,272) | Volpini et al., 2002; Klotz et al., 2007 |
| NECA | 14 | 20 | 140 | 25 | NS | Fredholm et al., 2011 |
| CV 1808 | 600 | 76 | >50,000a | 1450 | A2A (8 to >658) | Trivedi and Bruns, 1989; Kull et al., 1999; Brackett and Daly, 1994; Varani et al., 1998 |
| Antagonists | ||||||
| SCH 442416 | >10,000 | 4.1 (0.05)b | >10,000 | >1000 | A2A (250 to >2500) | Shinkre et al., 2010; Todde et al., 2000 |
| PSB 603 | >10,000 | >10,000 | 0.6 | >10,000 | A2B (>16,667) | Borrmann et al., 2009 |
NS, nonselective.
↵a EC50 for cAMP accumulation in murine NIH 3T3 fibroblasts.
↵b There are conflicting data on the affinity of SCH 442416 for the adenosine A2A-receptor. The Ki value shown in parentheses was reported by Todde et al. (2000), which is 82-times lower than that found by Shinkre et al. (2010).