| Bioactivity | 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[1]. | |||||||||
| Invitro | 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[1]. JNJ-5207787 (10 μM; 15 min) inhibits [125I]PYY labeling in lateral septum, cerebellum, ventral tegmental area, substantia nigra, hippocampus, septum, amygdala, and hypothalamus[1]. | |||||||||
| In Vivo | JNJ-5207787 (i.p.; 30 mg/kg) penetrates into the brain (Cmax=1351 ng/ml at 30 min) and occupies Y2 receptor binding sites[1]. Animal Model: | |||||||||
| Name | JNJ-5207787 | |||||||||
| CAS | 683746-68-1 | |||||||||
| Formula | C32H38N4O2 | |||||||||
| Molar Mass | 510.67 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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 |
JNJ-5207787
CAS: 683746-68-1 F: C32H38N4O2 W: 510.67
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist
Data collection：peptidedb@qq.com
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