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

KiSelectivity (Fold)Reference(s)
 (±)5′-Cl-5′-deoxy-ENBA0.5134027401290A1 (2418–5480)Franchetti et al., 2009
 CGS 2168028927361,00067A2A (2–13,370)Klotz et al., 1998
 Bay 60-6583>10,000>10,0003.0>10,000A2B (>3333)Kuno et al., 2007
 HEMADO3271230>300001.1A3 (297 to >27,272)Volpini et al., 2002; Klotz et al., 2007
 NECA142014025NSFredholm et al., 2011
 CV 180860076>50,000a1450A2A (8 to >658)Trivedi and Bruns, 1989; Kull et al., 1999; Brackett and Daly, 1994; Varani et al., 1998
 SCH 442416>10,0004.1 (0.05)b>10,000>1000A2A (250 to >2500)Shinkre et al., 2010; Todde et al., 2000
 PSB 603>10,000>10,0000.6>10,000A2B (>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).