Table 5.
The PK profiles of selected analogs in CD-1 mice.
| Cpd. | administrationa | t1/2 (h) | Cmax (ng/mL)b | AUC0−∞ (h●ng/mL) | Vss (L/kg) | CLp (mL/min/kg) | F% |
|---|---|---|---|---|---|---|---|
| 34 | po (10 mg/kg)c | 4.0 | 9 | 54 | |||
| 48 | po (10 mg/kg)d | BLOQe | |||||
| 65 | iv (2 mg/kg)f | 3.1 | 1690 | 1757 | 1.7 | 19.8 | |
| 65 | po (10 mg/kg)f | 2.1 | 934 | 4494 | 51 |
n= 3, iv and po represents intravenous and oral administration, respectively.
The maximum drug concentration (Cmax) was observed at t = 5 min, the first sampling time point after iv administration.
The compound was formulated as a solution in PEG400/water (1/3).
The compound was formulated as a solution in 20% HP-β-CD in water.
BLOQ: below limit of quantitation.
The compound was formulated as a solution in 30% solutol in water and adjusted pH with 1.05 equiv of HCl using 0.1 N HCl(aq).