Table III.
Inhibitory effect of various compounds on pregabalin uptake by hCMEC/D3 cells
| Compound | Uptake (% of Control) | |
|---|---|---|
| Control | 100 ± 5 | |
| Na+ − free | 102 ± 7 | |
| 1 mM | BCH | 17.0 ± 3.0* |
| 1 mM | L-Leu | 16.7 ± 2.7* |
| 1 mM | L-His | 20.6 ± 1.0* |
| 1 mM | L-Phe | ULQ (< 6.15) |
| 1 mM | L-Trp | ULQ (< 5.66) |
| 10 μM | JPH203 | ULQ (< 6.53) |
| 1 mM | L-Glu | 117 ± 6 |
| 1 mM | L-Arg | 101 ± 2 |
| 10 mM | MeAIB | 80.8 ± 4.0* |
| 1 mM | TEA | 89.8 ± 4.3 |
| 1 mM | PAH | 115 ± 7 |
hCMEC/D3 cells were incubated with pregabalin (10 μM) in the presence or absence (Control) of various compounds at 37°C for 10 min. Each value represents the mean ± SEM (n = 4–12). The uptake in the presence of 1 mM L-Phe, 1 mM L-Trp, or 10 μM JPH203 was below lower limit of quantification. ULQ means under the limit of quantification. The value in parentheses following ‘ULQ’ represents the value of the quantification limit. *p < 0.05, significantly different from control