Table 4.
[3H]-MPP+ uptake inhibition by [H2L1−4]Cl and 1–4 in HEK OCT1–3 cells.
| Compound | OCT1 (IC50, μM) [a] |
OCT2 (IC50, μM) [a] |
OCT3 (IC50, μM) [a] |
|---|---|---|---|
| [H2L1]Cl | 740.2 ± 194.8 | >4000 | 105.1 ± 32.8 |
| [H2L2]Cl | 390.8 ± 40.0 | >4000 | 102.8 ± 23.4 |
| [H2L3]Cl | 168.6 ± 26.2 | 236.2 ± 97.1 | 63.1 ± 8.9 |
| [H2L4]Cl | 118.9 ± 50.0 | 370.8 ± 123.2 | 27.8 ± 5.0 |
| 1 | 268.6 ± 31.5 | 8.5 ± 0.9 | 6.6 ± 1.9 |
| 2 | 113.4 ± 21.8 | 7.6 ± 0.2 | 2.4 ± 0.4 |
| 3 | 32.2 ± 2.9 | 4.0 ± 0.3 | 1.3 ± 0.5 |
| 4 | 0.25 ± 0.08 | 0.20 ± 0.02 | 0.62 ± 0.27 |
| D-22 [b] | 0.98 ± 0.31 | 1.13 ± 0.19 | 0.09 ± 0.01 |
| Prazosin [b] | 1.84 ± 0.48 | >100 | 12.6 ± 2.93 |
| Corticosterone [b] | 21.7 ± 2.44 | 34.2 ± 6.47 | 0.29 ± 0.04 |
[a] IC50 values derived from concentration-response curves. IC50 values are quoted with their standard deviations (SD). Values are mean ± SD of 3–4 independent experiments performed in triplicates. [b] IC50 values were taken from ref. [33].