TABLE 5

Exposure measures and brain penetration of WAY-132983

Male Sprague-Dawley rats were dosed with a single intraperitoneal injection of WAY-132983. Plasma and brain samples were taken and processed as described under Materials and Methods. Data shown are the mean of three rats. The brain/plasma ratio was determined from the AUC data.

Dose Matrix CmaxTmax AUClast Brain/Plasma Ratio
ng/ml or g h h ยท ng/ml or g
0.1 mg/kg Brain 79 1.0 217 24.1
Plasma 3 1.0 9
0.3 mg/kg Brain 247 0.5 717 32.6
Plasma 14 0.5 22
1.0 mg/kg Brain 1185 1.0 3058 33.2
Plasma 45 0.5 92