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Figure 3 | BMC Neuroscience

Figure 3

From: The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold

Figure 3

Sleep efficacy of DORA-12 in rats is associated with OX 2 R occupancies between 63 and 83%. A. Attenuation of mean time in active wake in rats in response to DORA-12 (1 mg/kg [n = 14], 3 mg/kg [n = 14], 10 mg/kg [n = 8], and 30 mg/kg [n = 14) relative to vehicle (20% Vitamin E TPGS, p.o.) dosed mid-active phase (arrow). Gray shading, dark period. 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). Maximum plasma values (Cmax) and corresponding occupancy values determined in satellite animals are listed to the right. B. The mean percent change (± SEM) in active wake quantified from individual PSG recordings from ‘A’ versus percent OX2R occupancy determined in rats (satellite animals). Light and dark shading indicates potential and definitive occupancy ranges. *** P < 0.001 (t-test) difference in percent active wake change versus baseline.

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