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.

OX2 recepter (human):700 nM (Ki), OX1 receptor:85 ng/mL (EC50), OX1 receptor (human):16 nM (Ki)

JNJ-5471779, administered orally at a dosage of 30 mg/kg for 6 hours, markedly decreases the onset time of rapid eye movement (REM) sleep and extends the duration spent in REM sleep. Additionally, when given at dosages ranging from 3 to 30 mg/kg, it effectively diminishes bradycardia responses. Moreover, at a 5 mg/kg oral dosage, JNJ-5471779 exhibits low clearance rates. These findings were observed in OX2R KO mice and rats for the sleep and bradycardia studies, respectively, and in mice for the pharmacokinetic analysis.