Author/Authors :
Cheryl P. Kordik، نويسنده , , Chi Luo، نويسنده , , Brian C. Zanoni، نويسنده , , Timothy W. Lovenberg، نويسنده , , Sandy J. Wilson، نويسنده , , Anil H. Vaidya، نويسنده , , Jeffrey J. Crooke، نويسنده , , Daniel I. Rosenthal، نويسنده , , Allen B. Reitz، نويسنده ,
Abstract :
1-Aryl-3-carboxamido-5-alkylpyrazoles were prepared based on a hit found in high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. 1-(3-Trifluoromethylphenyl)-3-[N-(5-quinolinyl)carboxamido]-5-methylpyrazole (31) bound to the human neuropeptide Y5 receptor with a 80 nM IC50 and was shown to inhibit cumulative food consumption 43.2% 2–6 h after ip dosing in a fasting-induced feeding model in rats.