Table 1. Inhibition of Drugs at hDAT, hSERT, and hNET in HEK293 Cells as Determined in Uptake Assays.
Drugs | DAT uptake, Ki, nM, [3H]DA a | SERT uptake, Ki, nM, [3H]5-HTa | NET uptake, Ki, nM [3H]DAa |
D-142 | 179±27 | 5.43±1.40 | 21.2±4.3 |
D-473 | 70.4±16.7 | 9.18±1.69 | 39.7±7.6 |
Fluoxetine | 5,126±3,260 | 14.4+1.1 | 1,755±444 |
Desipramine | 4,051±1,029 | 57.3±10.2 | 0.86±.04 |
Citalopram | 3.66±0.64 | ||
Benztropine | 90±16b | ||
GBR 12909 | 22.3±4.4 | 780±195 | 261±112 |
Uptake into cells expressing hDAT, hSERT, or hNET was measured as described in Methods. Where indicated (superscript b), values are from our previous publication. Results are average±S.E.M. for 3 to 10 independent determinations.
Chen et al., 2004.