Table VII.
Single-Dose Plasma and Brain Pharmacokinetics of IND24, IND81, and Compd B in Female FVB Mice. Intravenous (IV) Dose was 1 mg/kg; Dose by Oral Gavage (PO) was 10 mg/kg. Mean ± SD Shown for Cmax and AUC Value (n = 2)
| Compd | Route/Matrix | Vss (L/kg) | CL (L/h/kg) | t1/2 (h) | Cmax (μM) | tmax (h) | AUClast (μM*h) | %F | Brain/Plasma AUClast Ratio |
|---|---|---|---|---|---|---|---|---|---|
| IND24 | IV/Plasma | 2.46 | 0.92 | 2.16 | 2.49±2.65 | 0.083 | 2.78±1.09 | – | – |
| PO/Plasma | – | – | 4.65 | 1.66±0.11 | 2 | 11.2±1.31 | 40.3 | – | |
| PO/Brain | – | – | nd | 2.45±0.74 | 4 | 29.1±1.24 | – | 2.60 | |
| IND81 | IV/Plasma | 12.6 | 9.05 | 1.18 | 0.52±0.28 | 0.083 | 0.30±0.04 | – | – |
| PO/Plasma | – | – | 0.98 | 0.43±0.03 | 0.5 | 0.82±0.39 | 27.3 | – | |
| PO/Brain | – | – | 1.46 | 1.62±0.54 | 0.5 | 4.54±2.28 | – | 5.53 | |
| Compd B | IV/Plasma | 1.53 | 4.56 | 0.22 | 1.76±0.14 | 0.083 | 0.83±0.12 | – | – |
| PO/Plasma | – | – | 1.01 | 0.83±0.38 | 0.5 | 2.06±0.06 | 24.8 | – | |
| PO/Brain | – | – | nd | 0.46±0.16 | 2 | 1.06±0.10 | – | 0.51 |