Effect of OCT inhibitors on imatinib uptake by CEM cells
Inhibitor . | Inhibitor concentration, μM . | Imatinib uptake, ng/million cells . | Comments . |
|---|---|---|---|
| Verapamil | Control | 133.9 (25.3) | Known to inhibit hOCT125 |
| 5 | 125.9 (29.7) | ||
| 10 | 110.3 (27.9) | ||
| 50 | 65.5 (26.1) | ||
| 100 | 52.4 (22.5)* | ||
| 500 | 10.9 (2.7)* | ||
| Amantadine | Control | 284.2 (48.6) | Inhibits hOCT1 and hOCT226 |
| 50 | 284.8 (47.2) | ||
| 100 | 211.8 (42.8) | ||
| 500 | 56.6 (8.3)* | ||
| 1000 | 39.4 (1.9)* | ||
| 5000 | 24.5 (2.4)* | ||
| Procainamide | Control | 156.8 (12.6) | Inhibits hOCT1 and hOCT226 |
| 1 | 182.8 (8.8) | ||
| 10 | 175.6 (6.8) | ||
| 100 | 136.0 (5.6) | ||
| 1000 | 89.1 (3.5)* | ||
| 10 000 | 59.9 (2.2)† | ||
| Prazosin | Control | 228.6 (32.3) | Inhibits hOCT1 and hOCT327 |
| 0.01 | 235.1 (31.3) | ||
| 0.1 | 222.5 (36.2) | ||
| 1 | 224.8 (26.9) | ||
| 10 | 136.5 (20.2) | ||
| 100 | 29.4 (5.0)* | ||
| Corticosterone | Control | 162.7 (37.3) | Inhibits hOCT327 |
| 0.001 | 178.7 (31.9) | ||
| 0.01 | 178.1 (34.6) | ||
| 0.1 | 175.4 (33.4) | ||
| 1 | 162.8 (34.9) | ||
| 10 | 171.4 (37.0) | ||
| N-methylnicotinamide | Control | 150.1 (30.7) | Inhibits hOCT2 at nanomolar and micromolar concentrations28 |
| 1 | 154.7 (26.9) | ||
| 10 | 166.8 (30.2) | ||
| 100 | 145.0 (22.4) | ||
| 1000 | 156.8 (27.8) | ||
| 10 000 | 114.3 (16.6) |
Inhibitor . | Inhibitor concentration, μM . | Imatinib uptake, ng/million cells . | Comments . |
|---|---|---|---|
| Verapamil | Control | 133.9 (25.3) | Known to inhibit hOCT125 |
| 5 | 125.9 (29.7) | ||
| 10 | 110.3 (27.9) | ||
| 50 | 65.5 (26.1) | ||
| 100 | 52.4 (22.5)* | ||
| 500 | 10.9 (2.7)* | ||
| Amantadine | Control | 284.2 (48.6) | Inhibits hOCT1 and hOCT226 |
| 50 | 284.8 (47.2) | ||
| 100 | 211.8 (42.8) | ||
| 500 | 56.6 (8.3)* | ||
| 1000 | 39.4 (1.9)* | ||
| 5000 | 24.5 (2.4)* | ||
| Procainamide | Control | 156.8 (12.6) | Inhibits hOCT1 and hOCT226 |
| 1 | 182.8 (8.8) | ||
| 10 | 175.6 (6.8) | ||
| 100 | 136.0 (5.6) | ||
| 1000 | 89.1 (3.5)* | ||
| 10 000 | 59.9 (2.2)† | ||
| Prazosin | Control | 228.6 (32.3) | Inhibits hOCT1 and hOCT327 |
| 0.01 | 235.1 (31.3) | ||
| 0.1 | 222.5 (36.2) | ||
| 1 | 224.8 (26.9) | ||
| 10 | 136.5 (20.2) | ||
| 100 | 29.4 (5.0)* | ||
| Corticosterone | Control | 162.7 (37.3) | Inhibits hOCT327 |
| 0.001 | 178.7 (31.9) | ||
| 0.01 | 178.1 (34.6) | ||
| 0.1 | 175.4 (33.4) | ||
| 1 | 162.8 (34.9) | ||
| 10 | 171.4 (37.0) | ||
| N-methylnicotinamide | Control | 150.1 (30.7) | Inhibits hOCT2 at nanomolar and micromolar concentrations28 |
| 1 | 154.7 (26.9) | ||
| 10 | 166.8 (30.2) | ||
| 100 | 145.0 (22.4) | ||
| 1000 | 156.8 (27.8) | ||
| 10 000 | 114.3 (16.6) |