Pharmacokinetic parameters |
AUC (ng/ml · hr) | 299 ± 71 | 329 ± 58 | 3893 ± 514 | 18050 ± 1600 |
C
max (ng/ml) | 403 ± 105 | 29.2 ± 6.0 | 1392 ± 181 | 2027 ± 72 |
T
max(hr) | 0.081-b
| 2.4 ± 1.3 | 0.081-b
| 1.5 ± 0.22 |
Rate constants1-c
| 5.46 ± 0.67 | 0.45 ± 0.111-d
| 0.35 ± 0.03 | 2.34 ± 0.531-d
|
| 0.85 ± 0.13 | 0.33 ± 0.09 | 0.042 ± 0.01 | 0.137 ± 0.008 |
| 0.08 ± 0.01 | 0.042 ± 0.011 | – | 0.036 ± 0.021 |
Pharmacodynamic parameters |
Effect-compartment model |
CE50 (nM) | 3.7 ± 1.0 | 0.56 ± 0.1 | 18.8 ± 2.5 | 38.4 ± 10.9 |
K
e0 (hr−1) | 0.17 ± 0.02 | 0.34 ± 0.07 | 0.50 ± 0.07 | 1.4 ± 0.2 |
E
max(%) | 90.1 ± 1.1 | 90.8 ± 3.1 | 87.6 ± 1.6 | 90.8 ± 2.7 |
n (Hill) | 1.94 ± 0.81 | 1.92 ± 0.36 | 1.92 ± 0.89 | 1.30 ± 0.52 |
Indirect pharmacodynamic model1-e |
CE50(nM) | 0.43 | 0.39 | 9 | 31 |
K
out(hr−1) | 0.18 | 0.17 | 0.2 | 0.2 |
n(Hill) | 3.88 | 1.53 | 1.48 | 1 |