Table 3.
Inhibition of OCT(N) Function
| Agent | OCT1 | OCT3 | OCTN1 | OCTN2 |
|---|---|---|---|---|
| Amiodarone | 72.5 ± 10.5⁎ | 87.5 ± 20.5 | 68 ± 10 | 66.3 ± 16.2⁎ |
| Atenolol | 81.8 ± 10.8⁎ | 99.1 ± 27.2 | 80.1 ± 10.9 | 99.5 ± 3.3 |
| Atorvastatin | 69.5 ± 16.3⁎ | 72.9 ± 11.6⁎ | 98.4 ± 28.4 | 88.0 ± 5.4⁎ |
| Atropine | 16.9 ± 3.0⁎ | 106.5 ± 8.6 | 18.8 ± 21.3⁎ | 86.8 ± 22.4 |
| Bisoprolol | 62.8 ± 9.3⁎ | 94.0 ± 13.3 | 91.1 ± 16.6 | 93.4 ± 6.6 |
| Carvedilol | 6.7 ± 3.0⁎ | 75.3 ± 13.6⁎ | 29.8 ± 16.3⁎ | 91.8 ± 12.2 |
| Digoxin | 53.8 ± 8.4⁎ | 87.2 ± 4.6⁎ | 91.5 ± 29.7 | 92.3 ± 8.3 |
| Diltiazem | 7.2 ± 2.9⁎ | ND | 30.7 ± 18.0⁎ | ND |
| Flecainide | 18.5 ± 5.3⁎ | 83.8 ± 7.4⁎ | 32.4 ± 16.8⁎ | 98.1 ± 68.5 |
| Ipratropium bromide | 11.5 ± 0.7⁎ | 76.9 ± 1.7⁎ | 32.3 ± 8.8⁎ | 71.3 ± 2.3⁎ |
| Lidocaine | 52.2 ± 4.2⁎ | 85.2 ± 10.8⁎ | 37.5 ± 5.3⁎ | 77.6 ± 7.8⁎ |
| Metoprolol | 32.7 ± 5.7⁎ | 87.2 ± 24.6 | 86.9 ± 10.6 | 95.8 ± 15.0 |
| Molsidomine | 87.1 ± 5.3⁎ | 84.6 ± 12.2⁎ | 96.8 ± 19.1 | 92.7 ± 24.3 |
| Nadolol | 58.2 ± 16.3⁎ | 112.1 ± 19.3 | 101.1 ± 12.8 | 93.3 ± 9.0 |
| Nifedipine | 15.7 ± 8.1⁎ | 35.4 ± 17.5⁎ | 6.3 ± 5.7⁎ | 69.6 ± 16.4⁎ |
| Propafenone | 14.1 ± 5.6⁎ | 56.2 ± 4.3⁎ | 32.8 ± 17.9⁎ | 86.7 ± 15.4 |
| Propranolol | 12.8 ± 6.7⁎ | 12.6 ± 4.1⁎ | 41.1 ± 9.2⁎ | 78.9 ± 5.5⁎ |
| Sotalol | 86.2 ± 10.1 | 91.8 ± 22.8 | 91.9 ± 22.0 | 90.2 ± 17.3 |
| Spironolactone | 9.8 ± 4.6⁎ | 72.9 ± 6.5⁎ | 32.6 ± 11.2⁎ | 72.2 ± 12.0⁎ |
| Talinolol | 29.2 ± 4.5⁎ | 79.9 ± 21.1 | 89.3 ± 13.8 | 90.8 ± 5.7⁎ |
| Verapamil | 7.0 ± 3.5⁎ | 22.9 ± 14.8⁎ | 8.5 ± 7.0⁎ | 66.5 ± 38.3 |
Cells were incubated with radiolabeled standard substrates in the presence of various drugs (100 μmol/L) as described in Materials and Methods. Values (mean ± SD) represent the percentage of residual transport activity compared with solvent control. ND, not determined.
⁎
P < 0.05, Student's t-test.