Table 1.
S2116 | S2157 | |
---|---|---|
(±)-trans | (±)-trans | |
Cmax (μM) | 3.77 ± 0.56 | 4.33 ± 3.07 |
T1/2 (h) | 10.88 ± 2.97 | 0.88 ± 0.04 |
AUC (μM•h) | 41.78 ± 8.66 | 5.75 ± 3.67 |
nAUC (μM•h)** | 0.84 ± 0.17 | 0.11 ± 0.07 |
Plasma concentration at 0.5 h (μM) | 8.17 ± 2.80 | 5.71 ± 2.47 |
Brain concentration at 0.5 h (μmol/kg) | 1.35 ± 0.39 | 64.0 ± 3.46 |
Brain/Plasma ratio | 0.17 ± 0.03 | 13.0 ± 6.26 |
Pharmacokinetic parameters were determined in NOD.CB17-PrkdcSCID/J mice treated with a single intraperitoneal injection of either S2116 or S2157 in 5 mL of 6.25% DMSO-saline at 50 mg/kg (n = 3).
Dose-normalized AUC