Table II.
Inhibitory effect of pregabalin on LAT1 and LAT2-mediated amino acid uptake
| [14C]L-Leucine uptake (μL/mg-protein) | Transporter-mediated [14C]L-leucine uptake (μL/mg-protein) | |||
|---|---|---|---|---|
| Control | + 1 mM pregabalin | Control | + 1 mM pregabalin | |
| Mock | 247 ± 5 | 66.4 ± 4.5* | – | – |
| LAT1 | 485 ± 29 | 103 ± 7* | 237 ± 29 [100] | 36.8 ± 8.5* [15.5] |
| LAT2 | 345 ± 13 | 192 ± 7* | 97.8 ± 14 [100] | 126 ± 6 [129] |
LAT1-, LAT2-overexpressing, and mock cells were incubated with [14C]L-leucine (0.4 μM) in the presence or absence (Control) of 1 mM pregabalin at 37°C for 2 min. Transporter-mediated uptake was calculated by subtracting the uptake by mock cells from that by LAT-overexpressing cells. Values in square brackets represent percentage of control uptake. Each value represents the mean ± SEM (n = 3). *p < 0.05, significantly different from control