Table 2.
MI-4 binding and substrate uptake inhibition at HEK-hDAT, HEK-hSERT and HEK-hNET cellsa
| HEK-hDAT cells | MI-4 | Cocaine |
|---|---|---|
| [125l]-RTI-55 binding (Ki, nM) | 3460 ± 260 | 167 ± 25 |
| Hill coefficient | -0.80 ± 0.10 | -0.81 ± 0.03 |
| [3H]-Dopamine uptake (IC50, nM) | 6800* | 304 ± 55 |
| HEK-hSERT cells | ||
| [125l]-RTI-55 binding (Ki, nM) | 670 ±100 | 294 ± 83 |
| Hill coefficient | -1.09 ± 0.04 | -1.12 ± 0.03 |
| [3H]-Serotonin uptake (IC50, nM) | 790 ±170 | 390 ±140 |
| HEK-hNET cells | ||
| [125l]-RTI-55 binding (Ki, nM) | 365 ± 68 | 188 ± 96 |
| Hill coefficient | -1.04 ± 0.07 | -0.71 ± 0.06 |
| [3H]-NE uptake (IC50, nM) | 2090 ± 280 | 286 ± 50 |
a
Values represent the mean ± SEM from at least three independent experiments, each conducted in duplicate (for binding assays) or triplicate (for uptake assays) determinations. For MI-4 inhibition of dopamine uptake, some experiments yielded Ki values greater than 10 μM; these were assigned a value of 10 μM to allow calculation of an average. The actual value is greater than the average, and no standard error is reported.