Inhibitor and substrate sensitivity of frog catecholamine (fET) and human norepinephrine (hNET) transporter
| Agent | Ki orKm(nm) | |
|---|---|---|
| fET | hNET | |
| Mazindol | 0.22 ± 0.02 | 0.20 ± 0.03 |
| Desipramine | 0.82 ± 1.5 | 0.53 ± 0.06 |
| Imipramine | 2.2 ± 0.9 | 8.7 ± 3.5 |
| Mianserin | 2.5 ± 0.03 | 2.3 ± 0.3 |
| RTI-55 | 6.7 ± 1.3 | 4.4 ± 0.9 |
| Nomifensine | 6.8 ± 1 | 3.3 ± 0.4 |
| Nortriptyline | 11.4 ± 3 | 7.0 ± 2.0 |
| Clomipramine | 14 ± 2 | 27 ± 4 |
| Amytriptyline | 22 ± 4 | 44 ± 7 |
| Dopamine | 34 ± 7 | 180 ± 46* |
| d-Amphetamine | 42 ± 8 | 57 ± 1 |
| Paroxetine | 71 ± 10 | 153 ± 23 |
| l-Amphetamine | 85 ± 12 | 65 ± 9 |
| Cocaine | 160 ± 24 | 76 ± 11 |
| n-Methyldopamine | 301 ± 48 | 320 ± 22 |
| GBR 12909 | 320 ± 48 | 320 ± 22 |
| l-Norepinephrine | 460 ± 71 | 686 ± 50 |
| Iprindole | 832 ± 90 | 1313 ± 110 |
| l-Epinephrine | 998 ± 167 | 4424 ± 752* |
| 5-HT | 20,000 | 10,000 |
Ki or Km values for different agents were determined from inhibiiton curves obtained by [3H]-l-norepinephrine uptake assays performed on transfected cells in parallel. Data are presented as mean ± SEM of three separate experiments. Asterisks indicate statistically different potency for hNET as compared with fET (p < 0.05; Student’s unpaired t test).