Binding, uptake, and release in hSERT cells
| Drug | Binding Ki4-a | Uptake IC50b | Release IC50c | Maximum Stimulated Release |
|---|---|---|---|---|
| nM | nM | nM | % | |
| AMPH | 37,700 ± 1,520 | 1,867 | 224.2 | 59 |
| METH | 21,200 ± 10,500 | 25,137 ± 6957 | 252.7 | 58 |
| AMPH NHOH | >10,000 | >10,000 | 1315 | 47 |
| AMPH oxime | >10,000 | >10,000 | 1640 | 29 |
| METH NHOH | >10,000 | >10,000 | 2791 | 15 |
↵4-a drug inhibition of [125I]RTI-55 binding in HEK-hSERT cell membranes; b drug inhibition of [3H]5HT uptake in HEK-hSERT cells; c drug-mediated release of [3H]MPP+ from C-6-hSERT cells. Values are mean ± S.E.M. for three to four experiments.