TABLE 4

Agonist activation of wild-type and mutant adenosine A2A receptor cAMP production by HEK293T cells stably expressing wild type or transiently transfected with D52A2.50, S91A3.39, W246A6.48, N280A7.45, or N284A7.49 hA2AAR, was measured in presence of increasing concentrations of CGS21680

pEC50 and % response values are means ± S.E.M. of at least three separate assays performed in triplicate.

CGS21680
pEC50 (EC50a)Changeb%Responsec
Wild type7.8 ± 0.0 (17)1.0100 ± 14
D52A2.50N.D.dN.D.d−2 ± 1***
S91A3.39N.D.eN.D.e27 ± 11***
W246A6.487.1 ± 0.0*** (86)5.146 ± 13**
N280A7.457.8 ± 0.1 (17)1.029 ± 12***
N284A7.49N.D.dN.D.d2 ± 2***
  • a EC50 (nM) in parentheses.

  • b Change in fold over wild type.

  • c %Signaling response of receptor to CGS21680 (EmaxEbasal) in % of wild-type response.

  • d No stimulation of cAMP was observed with 10 µM CGS21680.

  • e Basal activity was too high to determine an accurate EC50 value.

  • Significantly different from wild-type with **P < 0.01 or ***P < 0.001 (one-way analysis of variance with Dunnett’s posttest).