Figure 5.

Time course of DORA-12 and almorexant OX₂R occupancy and efficacy in rats. A (upper panels). The time course of DORA-12 (30 mg/kg) effects on active wake was determined in rats by telemetry PSG relative to vehicle (20% Vitamin E TPGS, p.o.) following treatment in active (n = 14) or inactive phase (n = 7). Time points at which significant differences exist between vehicle and DORA-12 responses are indicated by gray vertical lines and tick marks (short, medium, long marks: P < 0.05, 0.01, 0.001, respectively). B (upper panels). Effects of almorexant (100 mg/kg) on active wake relative to vehicle following treatment in active (n = 14) or inactive phase (n = 14). Lower panels. Plasma and CSF levels as well as OX₂R receptor occupancy of DORA-12 (A) and almorexant (B) following inactive phase treatment (one male, one female animal per time point). Plasma, CSF, and occupancy levels were determined in the same animals, in satellite to PSG experiments.