JNJ-5207787 is a penetrates the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. It is >100-fold selective versus human Y1, Y4, and Y5 receptors. JNJ-5207787 suppresses the binding of peptide YY with pIC50s of 7.0 and 7.1 for the human Y2 r

Y2 receptor (human):7.0 (pic50), Y2 receptor (rat):7.1 (pic50)

JNJ-5207787 (10 μM; 15 min) suppresses [125I]PYY labeling in the lateral septum, cerebellum, ventral tegmental area, substantia nigra, hippocampus, septum, amygdala, and hypothalamus. JNJ-5207787 (0.01, 0.1, 1, 10 μM) has antagonistic properties and suppresses the PYY-stimulated [35S]GTPγS binding to basal level with a p IC50 corr of 7.20 [1].

JNJ-5207787 (i.p.; 30 mg/kg) penetrates the brain (Cmax=1351 ng/ml at 30 min) and occupies Y2 receptor binding sites[1].