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. 2013 Mar 18;110(14):5480–5485. doi: 10.1073/pnas.1218165110

Fig. 3.

Fig. 3.

Experimental validation of predicted LAT-1 ligands. Predicted LAT-1 ligands were validated by cis-inhibition of gabapentin uptake. (A) Cells were coincubated with 12 predicted ligands and a positive control (BCH) at either 100 μM (filled bars) or 10 μM (open bars) concentrations and gabapentin (1 μM unlabeled and 10 nM radiolabeled). Each bar depicts the mean of two to four separate experiments; error bars represent SEM. (B and C) Dose-dependent inhibition of gabapentin (1 μM unlabeled with 10 nM radiolabeled) accumulation by 3,5-diiodo-L-tyrosine (IC50 = 7.9 μM) and acivicin (IC50 = 340 μM), respectively. Each point is the mean of two or three separate experiments; error bars represent SEM. Statistical analysis in A was by one-way ANOVA and Dunnett’s multiple comparison test. *P < 0.05.