Table 1

The K i values of tested compounds for [125I] I-AB-MECA (0.15 nM) binding to human A3adenosine receptors and the dissociation rates (k −1) in the absence and presence of the tested compounds (10 μM). The assay was carried out as described underExperimental Procedures. Data shown are the mean ±S.E. from three independent experiments performed in duplicate.

Ki(nM)k−1 (min−1)
nM
Control0.042  ± 0.007
VUF8501739  ± 1460.043  ± 0.004
VUF850296  ± 260.024  ± 0.0031-150
VUF8503581  ± 820.041  ± 0.011
VUF850417.3  ± 1.70.022  ± 0.0041-150
VUF8505307  ± 990.044  ± 0.012
VUF8507204  ± 420.021  ± 0.0021-150
VUF54551680  ± 6200.024  ± 0.0031-150
PD81723N.D.0.046  ± 0.009
CGS15943185  ± 370.045  ± 0.005
  • N.D., not determined.

  • 1-150p < 0.05 compared with control (Student's t test).