JNJ 5207787

Names

[ Name ]:
JNJ 5207787

[Synonym ]:
unii-ow44b6fa0y

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neuropeptide Y Receptor

[Target]

human Y2 receptor:7.0 (pIC50)

rat Y2 receptor:7.1 (pIC50)

[In Vitro]

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: Sixteen female Sprague-Dawley Rats (approximately 300 g of body weight)[1] Dosage: 30 mg/kg Administration: IP Result: Penetrated into the brain (Cmax=1351 ng/ml at 30 min) and occupied Y2 receptor binding sites.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₈N₄O₂

[ Molecular Weight ]:
510.67000

[ Exact Mass ]:
510.29900

[ PSA ]:
67.65000

[ LogP ]:
5.56128

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.