Table 1.
Pharmacokinetics of plasma PTBA, UPHD25, 36, 186, and 263 after intraperitoneal (ip) injection in mice
| Compound | Matrix | Route | Dose, mg/kg | Tmax, h | Cmax, ng/ml | AUC, h·g−1·ml−1 | T1/2, h |
|---|---|---|---|---|---|---|---|
| PTBA | Plasma | ip | 50 | 0.08 | 4,380.71 | 690.9 | 4.03 |
| UPHD25 | Plasma | ip | 50 | ND | ND | ND | ND |
| PTBA | 0.08 | 2,063.38 | 2,010.89 | 4.51 | |||
| UPHD36 | Plasma | ip | 50 | 0.08 | 10,380.57 | 10,753.71 | 3.82 |
| PTBA | 0.08 | 4,618.54 | 4,811.3 | 2.94 | |||
| UPHD186 | Plasma | ip | 50 | 0.08 | 4,659.77 | 15,32.21 | 0.23 |
| PTBA | 0.08 | 5,630.29 | 1,380.91 | 1.13 | |||
| UPHD263 | Plasma | ip | 50 | 0.08 | 1,031.42 | 366.9 | 1.13 |
| PTBA | ND | ND | ND | ND |
Male BALB/c mice were injected with PTBA analog at 50 mg/kg ip, and plasma samples were drawn at intervals over the next 8 h. ND, not determined. Parent compound and PTBA concentrations were determined in the plasma by LC-MS/MS. Cmax was determined at 0.08-h postinjection. The noncompartmental analysis module in Phoenix WinNonlin was used to derive AUC and T1/2 for the parent and PTBA metabolite. See text for other definitions.