Table 5. Pharmacokinetic Properties of Full Agonist 14a.
Compound | Species | Fu | oral dose (mg/kg) | oral AUC (μM·h) | Cl (L/h/kg) | Vdss (L/kg) | iv t1/2 (h) | % F |
---|---|---|---|---|---|---|---|---|
2 | rat | 0.010 | 2 | 15.1 | 0.91 | 1.1 | 1.8 | 72 |
14 | rat | 0.003 | 2 | 8.22 | 0.33 | 0.81 | 2.0 | 72 |
14 | dog | 0.034 | 2 | 11.6 | 0.21 | 0.68 | 4.1 | 62 |
2 | cyno | 0.012 | 10 | 18.8 | 0.81 | 2.0 | 2.1 | 71 |
14 | cyno | 0.017 | 10 | 80.4 | 0.22 | 0.5 | 3.3 | 91 |
Administered at a dose of 0.5 mg/kg, iv. Data are expressed as mean values (n = 3).