Table 2

Effects of two allosteric modulators on the inhibition of cyclic AMP production by three adenosine receptor agonists in intact CHO cells expressing human A3 receptors. MRS1220 (100 nM) was used to overwhelm the antagonistic activities of the allosteric modulators. The concentration of DU124183 and DU124482 used in the experiment was 10 μM. The accumulation level of cyclic AMP in CHO cells expressing human A3 receptors stimulated by 10 μM forskolin was 220 ± 30 nM (n = 5). Results were expressed as mean ± S.E.M. from three independent experiments.

EC50Cyclic AMP LevelMaximum Efficacy
nM nM % inhibition
C1-IB-MECA2.1  ± 0.4103  ± 853
+ MRS1220 (control)440  ± 60106  ± 1252
+ MRS1220 +DU124183210  ± 402-150 35  ± 62-150 84
+ MRS1220 + DU124482480  ± 50130  ± 112-150 41
MRS18981.9  ± 0.3108  ± 951
+ MRS1220 (control)350  ± 60106  ± 1052
+ MRS1220 + DU124183170  ± 402-150 42  ± 72-150 81
+ MRS1220 +DU124482370  ± 50132  ± 172-150 40
CADO (control)3700  ± 780108  ± 951
+ DU124183 (10 μM)N.D.48  ± 62-150 78
+ VUF5455 (10 μM)N.D.110  ± 1150
  • N.D., not determined.

  • 2-150P < 0.05 compared with control.