JNJ-54717793 is an orally active, brain-penetrating compound that acts as a selective and high-affinity antagonist of the orexin-1 receptor (OX1R) with a plasma EC50 of 85 ng/mL. It demonstrates K_i values of 16 nM for hOX1R (human OX1R) and 700 nM for hOX2R, indicating its strong preference for hOX1R over hOX2R. JNJ-54717793 is recognized for its effectiveness in the treatment of anxiety disorders.

JNJ-5471779 (30 mg/kg; p.o.; 6 hours) significantly reduces the latency for rapid eye movement (REM) sleep and increases the time spent in REM sleep [2]. JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses [2]. JNJ-5471779 (5mg/kg; p.o.) shows low clearance [1]. Animal Model: OX2R KO mice [2] Dosage: 30 mg/kg Administration: P.o. Result: Significantly reduced the latency for rapid eye movement (REM) sleep and prolonged the time spent in REM sleep. Animal Model: Rat [2] Dosage: 3~30 mg/kg Administration: P.o. Result: Attenuated bradycardia responses. Animal Model: Mouse [1] Dosage: 5.0 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Clearance was found to be low.