Table 3. PAMPA Permeability and Mouse PKa of 9b, 11b, and 11d.
PAMPA (nm/s) |
5 mg/kg iv dose |
25 mg/kg po dose |
||||
---|---|---|---|---|---|---|
pH 5.0 | pH 7.4 | Cl (mL/min/kg) | Vss (L/kg) | Cmax(μM) | F % | |
9b | 1090 | 1100 | 4 | 1.0 | 20.5 | 162 |
11b | 204 | 1050 | 7 | 1.2 | 3.1 | 18 |
11d | 145 | 672 | 21 | 4.9 | 1.9 | 27 |
Compounds were dosed as freebase in female CD-1 mice.