Pharmacological characterization of wild-type rat SERT and D98E mutant
| Drug | 5-HT uptake Ki or Km (nm unless otherwise indicated) | |
|---|---|---|
| rSERT | D98E | |
| Paroxetine | 0.3 ± 0.09 | 0.5 ± 0.14 |
| Mazindol | 272 ± 63 | 231 ± 62 |
| Cocaine | 390 ± 50 | 1490 ± 601-a |
| Imipramine | 38 ± 8 | 190 ± 70 |
| Citalopram | 2.2 ± 0.5 | 270 ± 901-a |
| 5-HT1-b | 460 ± 210 | 400 ± 160 |
| Na+ | 19.9 ± 2.3 mm | >100 mm1-a |
| Cl− | 5.2 ± 1.6 mm | 41.3 ± 2.5 mm |
Ki and Km values for various compounds for [3H]5HT uptake in HeLa cells transiently transfected with wild-type rSERT or the D98E mutant. [3H]5HT uptake experiments were performed as described in Materials and Methods. Data represent means ± SEs from results of three experiments performed in triplicate.
↵F1-a p < 0.05, compared with rSERT value.
↵F1-b Vmax values (mol/min per cell) for 5-HT transport determined in COS-7 cells were rSERT, 5.0 ± 2.4 × 10−18 and D98E, 2.4 ± 1.2 × 10−18.