Table 1.
The Ki values of tested compounds for [125I]I-AB-MECA (0.15 nM) binding to human A3 adenosine 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 under Experimental Procedures. Data shown are the mean ±S.E. from three independent experiments performed in duplicate.
Ki (nM) | k−1 (min −1) | |
---|---|---|
nM | ||
Control | 0.042 ± 0.007 | |
VUF8501 | 739 ± 146 | 0.043 ± 0.004 |
VUF8502 | 96 ± 26 | 0.024 ± 0.003* |
VUF8503 | 581 ± 82 | 0.041 ± 0.011 |
VUF8504 | 17.3 ± 1.7 | 0.022 ± 0.004* |
VUF8505 | 307 ± 99 | 0.044 ± 0.012 |
VUF8507 | 204 ± 42 | 0.021 ± 0.002* |
VUF5455 | 1680 ± 620 | 0.024 ± 0.003* |
PD81723 | N.D. | 0.046 ± 0.009 |
CGS15943 | 185 ± 37 | 0.045 ± 0.005 |
N.D., not determined.
p < 0.05 compared with control (Student's t test).