IC50 values (μM) of various compounds for the uptake of [14C]YM155 into hOCT1-HEK, hOCT2-HEK, human hepatocytes, and the human hormone refractory prostate cancer cell line PC-3
| hOCT1-HEK | hOCT2-HEK | Hepatocytea | PC-3b | |
|---|---|---|---|---|
| MPP | 30.4c | 4.42h | 16.7 | 824 |
| Cimetidine | 149d | 110i | 147 | 1412 |
| Tubocurarine | 62.4e | >100j | Not determined | 28.2 |
| Quinidine | 7.11e | 11.0e | Not determined | 3.62 |
| Prazosin | 1.56f | 80.4f | 1.43 | 4.27 |
| Corticosterone | 8.89e | 5.35e | 4.70 | >100 |
| Verapamil | 1.23f | 13.4e | Not determined | 4.38 |
| Amantadine | 39.6c | 45.9h | Not determined | 993 |
| Procainamide | 51.3c | 91.9c | Not determined | 987 |
| N-Methylnicotinamide | >1000g | ∼1000g | >1000 | 4209 |
↵a,b Values are cited from our previous studies by Iwai et al. (2009) and Minematsu et al. (2009), respectively. The substrate concentrations of YM155 (1 μM for hOCT1-HEK, hOCT2-HEK, and hepatocytes; 0.1 μM for PC-3) were set lower than the Km values of YM155 for hOCT1-HEK (22.1 μM), hOCT2-HEK (2.67 μM), hepatocytes (6.13–9.47 μM), and PC-3 (0.243 μM).
↵c Inhibitor concentrations: 0, 3, 10, 30, 100, 300, 1000, and 3000 μM.
↵d Inhibitor concentrations: 0, 20, 50, 100, 200, 500, 1000, and 2000 μM.
↵e Inhibitor concentrations: 0, 0.3, 1, 3, 10, 30, 100, and 300 μM.
↵f Inhibitor concentrations: 0, 0.1, 0.3, 1, 3, 10, 30, and 100 μM.
↵g Inhibitor concentrations: 1000 μM.
↵h Inhibitor concentrations: 0, 1, 3, 10, 30, 100, 300, and 1000 μM.
↵i Inhibitor concentrations: 0, 10, 30, 100, 300, 1000, 3000, and 10,000 μM.
↵j Inhibitor concentrations: 100 μM.