Table 3.
Total plasma concentration, calculated unbound plasma concentrations and unbound plasma concentration/IC50 (in vitro) of ADX71441 at the end of the experiment in female guinea pigs
| Treatment | Route | Dose (mg kg−1) | n | Total plasma exposure (ng mL−1) | Total plasma exposure (nM) | Unbound conc. (ng mL−1) | Unbound conc. (nM) | Unbound conc./EC50 (in vitro) |
|---|---|---|---|---|---|---|---|---|
| Vehicle | i.v. | 10 | ||||||
| ADX71441 | i.v. | 1 | 10 | 67 | 153 | 5.3 | 12.1 | 0.3 |
| ADX71441 | i.v. | 3 | 10 | 195 | 446 | 15.4 | 35.3 | 0.9 |
| Baclofen | i.v. | 6 | 10 |
Unbound plasma concentrations of ADX71441 were calculated from total plasma concentration using measured plasma protein binding in the guinea pig (fraction unbound = 7.9=).