Table 4. In Vivo Pharmacokinetics Profiles of 35, 49, and 52 in Ratsa.
IV (dose: 5 mg/kg) |
PO (dose: 20 mg/kg) |
||||||||
---|---|---|---|---|---|---|---|---|---|
comp. | T1/2 (h) | CL (mL/min/kg) | Vss (L/kg) | AUC(0-inf) (ng/mL·h) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) | AUC(0-inf) (ng/mL·h) | F (%) |
35 | 0.3 | 300 | 4.1 | 278 | ND | ND | ND | ND | ND |
49 | 2.9 | 60.6 | 4.7 | 1386 | 68.1 | 4.0 | 2.3 | 603 | 11 |
49S1 | 2.2 | 22 | 2.2 | 3912 | 253 | 1.7 | 2.3 | 2012 | 12.9 |
52S1 | 5.1 | 36.9 | 7.8 | 1967 | 255 | 0.3 | 6.9 | 2107 | 26.8 |
57S1 | 2.9 | 82.1 | 6.7 | 894 | ND | ND | ND | ND | ND |
S1 means the compound is a HCl salt; ND: not detected.