Summary of the IC50 values of various compounds against the uptake of [14C]YM155 into PC-3 and comparison with the IC50 values from the literature for human OCT1, OCT2, OCT3, OCTN1, OCTN2, and OCT6
IC50 | IC50a | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| OCT1 | OCT2 | OCT3 | OCTN1 | OCTN2 | OCT6 | |||||||
| μM | ||||||||||||
| d-Carnitine | >1000b | <2000 | 11c; 98c | 30 | ||||||||
| l-Carnitine | >1000b | 12,400 | 13,000 | 5590 | 24 | 4.3c; 4.8c | ||||||
| TEA | >1000b | 158; 173 | 48-270 | 1372 | ||||||||
| TBMEA | 458 | 66 | ||||||||||
| MPP | 824 | 12 | 2.4 | 54 | >1000 | >12,000 | >100 | |||||
| Cimetidine | 1412 | 166 | 70 | 17 | 435 | <2000 | ||||||
| Prazosin | 4.27 | 1.8 | >100 | 13 | ||||||||
| Corticosterone | >100 | 7; 22 | 34 | 0.12; 0.29 | ||||||||
| Quinidine | 3.62 | 18 | 69 | <100 | ||||||||
| Verapamil | 4.38 | 2.9 | 206 | 24 | 8.4 | <50 | ||||||
| Amantadine | 993 | 236 | 23 | >1000 | ||||||||
| Procainamide | 987 | 74; 107 | 50 | 738 | <500 | <3000 | <12,000 | |||||
| NMN | 4209 | 7700 | 270 | 3000 | 77 |
| <12,000 | |||||