Parameters determined from the fitting of the relationship between the PK and PD profiles after dosing of YM758 (0.3 mg/kg) to tachycardia-induced dogs
The time profiles of the plasma concentration of the unchanged drug and the HR reduction obtained after intravenous administration of YM758 to tachycardia-induced dogs were fitted according to the compartment model to obtain the parameters (PK: V and kel, PD: Emax, ECe50, and ke0). The details of the fitting procedure are described under Materials and Methods, and the data were taken mainly from Figs. 3, 4, 5.
Parameters | Estimated Values | S.E. |
|---|---|---|
| PK | ||
| V (l/kg) | 3.64 | 0.78 |
| kel (l/h) | 0.395 | 0.22 |
| PD | ||
| Emax (%) | 37.8 | 9.94 |
| ECe50 (ng/ml) | 6.0 | 4.2 |
| ke0 (l/h) | 0.048 | 0.024 |