Compound | Dose (mg/kg) | Plasma (nM) | OX2R Occa(% maxb) | Active wake reductionc% |
---|
Suvorexant | 10 | 1600.0 | 92.6 | -29.0*** |
 | 30 | 2100.0 | 94.3 | -79.6** |
 | 100 | 5100.0 | 97.6 | -79.9** |
DORA-12 | 0.3 | 20.2 | 34.0 | -7.9 |
 | 1 | 67.4 | 62.8 | -9.7 |
 | 3 | 202.2 | 83.0 | -28.8*** |
 | 10 | 674.0 | 93.9 | -44.2*** |
 | 30 | 2022.0 | 97.1 | -45.9*** |
- aOcc, occupancy.
- bNormalized occupancy was determined over a range of doses and fit to a one-sided binding hyperbolic curve to determine the maximum occupancy. OX2R occupancies corresponding to plasma values at indicated doses were calculated based on the normalized curve for each compound.
- cMean percent change in active wake relative to vehicle in the 2 h following treatment (**, ***, p < 0.01, 0.001, population t-test).