产品
编 号:F425775
分子式:C32H38N4O2
分子量:510.67
产品类型
结构图
CAS No: 683746-68-1
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产品详情
生物活性:
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.
体内研究:
JNJ-5207787 (i.p.; 30 mg/kg) penetrates into the brain (Cmax=1351 ng/ml at 30 min) and occupies Y2 receptor binding sites. Animal Model:Sixteen female Sprague-Dawley Rats (approximately 300 g of body weight)
Dosage:30 mg/kg
Administration:IP
Result:Penetrated into the brain (Cmax=1351 ng/ml at 30 min) and occupied Y2 receptor binding sites.
体外研究:
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.