NET and SERT uptake inhibition by duloxetine enantiomers
Cell-based study · NET- or SERT-overexpressing HEK293 cells with empty-vector controls [1]
Paired enantiomer uptake assay; Figure 7 reports mean ± SEM of three independent experiments. IC50 confidence intervals are reported separately in Table S6.
| Endpoint | Reported result | Reference |
|---|---|---|
| NET-mediated MPP+ uptake | IC50 R: 0.28 µM (95% CI 0.18–0.44); S comparator: 0.31 µM (95% CI 0.18–0.52) | [1] |
| SERT-mediated MPP+ uptake | IC50 R: 0.035 µM (95% CI 0.019–0.062); S comparator: 0.031 µM (95% CI 0.019–0.049) | [1] |
Literature-Reported Treatment Conditions
- Treatment concentration
- Increasing inhibitor concentrations; 0.2 µM MPP+ substrate
- Exposure duration
- 5 minutes
- Method
- Cellular uptake quantified by LC–MS/MS.
- Reported limits
- Vehicle for inhibitor stock not specified in the read Experimental Section. Table S1 gives neutral SMILES but does not explicitly identify the supplied counterion or enantiomeric purity; general test-compound purity is at least 95%.
Methods and source locations
Compound reported in the paper: (R)-Duloxetine; Compound label in the paper: TRC D720990; SI Table S1
Reported R-enantiomer cellular transport assay only.
Experimental Section; Figure 7B; SI Table S1 p2 and Table S6 p13
NET-mediated MPP+ uptake: LC–MS/MS; empty-vector uptake subtracted and activity normalized to uninhibited uptake. — Figure 7B and caption; SI Table S6 p13, NET duloxetine rows; Calculations
SERT-mediated MPP+ uptake: LC–MS/MS; matched empty-vector and uninhibited controls. — Figure 7B and caption; SI Table S6 p13, SERT duloxetine rows; Calculations