Table 1.
Plasma, unbound plasma concentrations and unbound plasma concentration/IC50 (in vitro) of ADX71441 at the end of the experiment in mice
| Treatment | Route | Dose (mg kg−1) | n | Plasma exposure (ng mL−1) | Plasma exposure (nM) | Unbound conc. (ng mL−1) | Unbound conc. (nM) | Unbound conc. EC50 (in vitro) |
|---|---|---|---|---|---|---|---|---|
| Vehicle | p.o. | 8 | ||||||
| ADX71441 | p.o. | 1 | 8 | 101 | 231 | 6 | 14 | 0.36 |
| ADX71441 | p.o. | 3 | 8 | 208 | 476 | 13 | 30 | 0.74 |
| ADX71441 | p.o. | 10 | 8 | 652 | 1493 | 40 | 93 | 2.31 |
| Oxybutynin | p.o. | 100 | 8 |
Unbound concentrations of ADX71441 were calculated from total plasma concentration using measured plasma protein binding in the mouse (fraction unbound = 6.2=).