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Figure 4 | BMC Neuroscience

Figure 4

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

Figure 4

Suvorexant efficacy in dogs corresponds to plasma exposures > 342 nM and OX 2 R occupancies > 65%. A. Suvorexant levels in satellite animals treated with suvorexant (1 or 3 mg/kg; p.o. in 20% Vitamin E TPGS) (n = 3, each time point). B. Calculated OX2R occupancy based on rat occupancy values, and normalized for free fraction of compound in rat (1.4%) and dog (1%). Gray shading indicates time points at which active wake was significantly attenuated in dogs treated with suvorexant (1 or 3 mg/kg), the plasma and occupancy range at which efficacy has been observed [12].

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