Table 4. Rat Pharmacokinetic Properties of Full Agonistsa.
Compound | Fu | oral Cmax (μM) | oral AUC (μM·h) | Cl (L/h/kg) | Vdss (L/kg) | iv t1/2 (h) | % F |
---|---|---|---|---|---|---|---|
8 | 0.006 | 0.37 | 1.74 | 0.67 | 1.12 | 2.1 | 29 |
4 | 0.006 | 0.25 | 1.83 | 0.72 | 1.68 | 2.0 | 34 |
14 | 0.003 | 1.18 | 8.22 | 0.33 | 0.81 | 2.0 | 72 |
18 | 0.003 | 0.36 | 2.43 | 0.49 | 1.9 | 3.3 | 32 |
Administered at a dose of 0.5 mg/kg, iv; 2 mg/kg, po, in rats. Data are expressed as mean values (n = 3).