Table 1:
IC50 values for inhibition of transporter-mediated uptake by FPM isomers in HEK293 cells. Values are given as mean ± SEM obtained from nonlinear curve fits obtained from n=3 independent experiments, performed in triplicate (data shown in Figure 2). DAT/SERT ratio is expressed as 1/(DAT IC50) divided by 1/(SERT IC50); higher values indicate greater selectivity for DAT. NET/SERT ratio is expressed as 1/(NET IC50) divided by 1/(SERT IC50); higher values indicate greater selectivity for NET. DAT/NET ratio is expressed as 1/(DAT IC50) divided by 1/(NET IC50); higher numbers indicate greater DAT-selectivity.
IC50 (µM) | ||||||
---|---|---|---|---|---|---|
DAT | NET | SERT | DAT / SERT ratio | NET / SERT ratio | DAT / NET ratio | |
2-FPM | 1.33 ± 0.09 | 1.29 ± 0.03 | 454 ± 15.4 | 340.1 | 351.4 | 0.97 |
3-FPM | 1.16 ± 0.29 | 1.51 ± 0.17 | 111.65 ± 13.08 | 96.4 | 73.7 | 1.31 |
4-FPM | 2.14 ± 0.39 | 2.05 ± 0.28 | 88.09 ± 1.83 | 41.2 | 42.9 | 0.96 |