| Description | 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 receptor and rat Y2 receptor, respectively. |
| In vitro | 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]. |
| In vivo | JNJ-5207787 (i.p.; 30 mg/kg) penetrates into the brain (Cmax=1351 ng/ml at 30 min). It also occupies Y2 receptor binding sites[1]. |
| Target activity | Y2 receptor (human):7.0 (pic50), Y2 receptor (rat):7.1 (pic50) |
| molecular weight | 510.67 |
| Molecular formula | C32H38N4O2 |
| CAS | 683746-68-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. 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 Mar;308(3):1130-7. |