Table 1.
Overview of the Specificity and Efficacy of the Pharmacological Inhibitors
| Inhibitors | LAT1 | LAT2 | MCT8 | MCT10 | OATP1A2 |
|---|---|---|---|---|---|
| BCH | ✓(146 μM) | ✓(∼100 μM) | X | X | X |
| L-tryptophan | ✓(17 μM) | ✓(45 μM) | X | ✓(>10 mM) | X |
| Verapamil | X | X | ✓(∼100 μM) | ✓(>100 μM) | ✓(1.5 μM) |
| Silychristin | X | X | ✓(0.12 μM) | X | ✓(>10 μM) |
| Rifampicin | X | X | X | X | ✓(50 μM) |
| Naringin | X | X | X | X | ✓(23 μM) |
The half maximal inhibitory concentration values of the inhibitors for the TH transporters were calculated using nonlinear curve fitting by GraphPad Prism 5 and depicted between brackets.
✓, inhibition; X, no inhibition; BCH, 2-amino-2-norbornanecarboxylic acid; LAT, L-type amino acid transporter; MCT, monocarboxylate transporter; OATP, organic anion transporting peptide; TH, thyroid hormone.