Inhibition of [3H]NBMPR binding
Cells were treated with MTS reagents and assessed for [3H]NBMPR binding in the presence and absence of a range of concentrations of test inhibitor as described for Fig. 3C. Each value is the mean ± S.E.M. from at least four independent experiments.
| Cell Line and Inhibitor | Ki | |
|---|---|---|
| Control | +MMTS | |
| nM | ||
| hENT1 | ||
| Dipyridamole | 22 ± 8 | 30 ± 9 |
| Draflazine | 3.3 ± 0.7 | 2.8 ± 0.9 |
| Dilazep | 1.9 ± 0.4 | 1.2 ± 0.6 |
| C87S | ||
| Dipyridamole | 71 ± 26* | N.D. |
| Draflazine | 4.6 ± 2.1 | N.D. |
| Dilazep | 4.5 ± 2.4 | N.D. |
| C193S | ||
| Dipyridamole | 32 ± 10 | 111 ± 32† |
| Draflazine | 3.5 ± 0.9 | 5.9 ± 1.2 |
| Dilazep | 5.2 ± 1.1* | 9.8 ± 4.2 |
| C213S | ||
| Dipyridamole | 22 ± 7 | 33 ± 11 |
| Draflazine | 2.2 ± 0.9 | 2.2 ± 0.8 |
| Dilazep | 2.6 ± 0.9 | 3.0 ± 1.3 |
| C222S | ||
| Dipyridamole | 32 ± 2 | 45 ± 14 |
| Draflazine | 3.2 ± 0.5 | 3.0 ± 0.7 |
| Dilazep | 3.2 ± 1.4 | 2.6 ± 0.8 |
N.D., not determined.
* P < 0.05, significantly different from the Ki determined in wild-type hENT1 (Student's t test for paired samples).
† P < 0.05, significantly different from control (Student's t test for paired samples).