JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y₂ receptor (Y₂) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC₅₀s of 7.0 and 7.1 for human Y₂ receptor and rat Y₂ receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y₁, Y₄, and Y₅ receptors.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Bonaventure P, et al. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide YY2 receptor. J Pharmacol Exp Ther. 2004  [Content Brief]