Table 1.
RTI-113 IC50 values for selected transporter mutants. One-way ANOVA was performed followed by Dunnett’s post-hoc analysis to see if the mNET mutants were significantly different from the wild type mNET.
| Transporter | RTI-113 IC50 [nM] uptake inhibition | Dunnett’s post-hoc versus mNET (n=3–6), p value |
|---|---|---|
| mNET | 170±25.3 | |
| mNET-TM8m | 269±35.8 | <0.05 |
| mNET-TM6m | 341±77.2 | <0.05 |
| mNET-TM3m | 1.89±1.29 | <0.001 |
|
| ||
| mDAT | 0.65±0.28 | <0.001 |
| mDAT F155Y | 13.4±1.9 | <0.001 (versus mDAT) |
|
| ||
| mNET Y151F | 12.1±0.8 | <0.001 |
| mNET Y151A | 130±15.1 | n/s |
| mNET Y151C | 211±23.0 | n/s |
| mNET Y151D | 306±105 | n/s |
| mNET Y151E | 770±55.3 | 0.001 |
| mNET Y151G | 165±28.4 | n/s |
| mNET Y151H | Low uptake | |
| mNET Y151I | 199±65.1 | n/s |
| mNET Y151K | 453±71.0 | <0.01 |
| mNET Y151L | 342±110 | n/s |
| mNET Y151M | 679±174 | <0.01 |
| mNET Y151N | 291±51.5 | n/s |
| mNET Y151P | Low uptake | |
| mNET Y151Q | 831±69.0 | <0.01 |
| mNET Y151R | Low uptake | |
| mNET Y151S | 99.3±43.8 | n/s |
| mNET Y151T | 115±33.2 | n/s |
| mNET Y151V | 181±81.1 | n/s |
| mNET Y151W | 256±66.9 | n/s |