Translational evaluation of novel selective orexin-1 receptor antagonist JNJ-61393215 in an experimental model for panic in rodents and humans

摘要

a Chemical structure of 3-fluoro-2-(pyrimidin-2-yl)phenyl)((1 S,4 R,6 R)-6-((5-(trifluoromethyl)pyridin-2-yl)oxy)-2-azabicyclo[2.2.1]heptan-2-yl-3,3-d2)methanone). b Ex vivo OX1R occupancy with JNJ-61393215 (10, 1, or 0.1 mg/kg, oral administration) in rat tenia tecta: time dependency. c Corresponding plasma and brain concentrations (n = 3 per time point and dose regimen, brain concentration at 0.1 mg/kg was not measured).