Table 2.
Striatal NK-1 receptor occupancy by aprepitant and plasma aprepitant concentrations in gerbils after oral aprepitant administration
Parameter | Dose | Time after administration | |||||
---|---|---|---|---|---|---|---|
0. 5 h | 1 h | 2 h | 4 h | 8 h | 24 h | ||
(n = 3) | (n = 3) | (n = 3) | (n = 3) | (n = 3) | (n = 5) | ||
Occupancy (%) | 0.3mg/kg | -4.54±3.10 | 48.8±8.60 | 91.4±1.20 | 95.2±0.72 | 93.0±0.34 | 67.5±3.31 |
3mg/kg | 90.6±0.84 | 98.7±0.21 | 99.3±0.32 | 99.0±0.71 | 99.2±0.26 | 93.5±1.19 | |
30mg/kg | 99.6±0.08 | 99.1±0.20 | 99.3±0.52 | 99.2±0.44 | 98.9±0.29 | 98.6±0.33 | |
Plasma Concentration (ng/mL) | 0.3mg/kg | 28.5±5.0 | 72.6±11.9 | 75.6±8.3 | 61.4±10.2 | 37.3±7.6 | 4.0±0.4 |
3mg/kg | 205.7±23.1 | 453.4±18.4 | 569.6±7.9 | 649.8±140.1 | 476.1±69.5 | 40.5±5.7 | |
30mg/kg | 2070.7±67.9 | 4438.0±441.9 | 6883.4±702.4 | 4949.7±409.7 | 4061.7±392.7 | 209.5±40.4 |
Data are expressed as mean ± SE.