Table 3. PK Parameters and Brain Tissue Exposurea.
brain/plasma ratio |
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compd | route | dose | CL (mL/min/kg) | VSS (L/kg) | t1/2 (h) | AUC (h·μM) | Cmax (μM) | F (%) | AUC | Cmax |
1 (WF-47-JS03) | iv | 5 | 51 | 13 | 3.9 | 3.2 | 1.1 | |||
pob | 20 | 11 | 12 | 0.73 | 94 | 0.94 | 0.81 | |||
9 (YA-14-WJ39) | iv | 5 | 54 | 7.8 | 1.8 | 2.6 | 1.6 | |||
po | 20 | 2.5 | 6.8 | 0.88 | 64 | 0.15 | 0.13 | |||
10 (SC-89-VU43) | iv | 2 | 19 | 5.1 | 3.7 | 2.8 | 0.94 | |||
po | 10 | 3.7 | 8.7 | 0.82 | 62 | NA | NA | |||
11 | iv | 2 | 110 | 11 | 1.6 | 0.49 | 0.45 | |||
po | 10 | 2.2 | 0.34 | 0.10 | 14 | NA | NA |
PK studies run in Balb/c mice.
HCl salt used for dosing.