| 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].
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| Related Catalog |
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| Target |
human Y2 receptor:7.0 (pIC50)
rat Y2 receptor:7.1 (pIC50)
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| 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].
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| 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.
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| 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.
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