Description
CGP 71683 is an antagonist of neuropeptide Y (NPY) receptor Y
5 (IC
50 = 1.4 nM in a radioligand binding assay). It is selective for Y
5 over Y
1, Y
2, and Y
4 receptors (IC
50s = 2,765, 7,187, and 5,637 nM, respectively). It inhibits NPY-induced increases in BT-549 cell growth and MDA-MB-231 cell migration when used at a concentration of 0.25 μM. CGP 71683 (10 mg/kg, i.p.) inhibits increases in food intake induced by intracerebroventricular administration of NPY in rats.
Biological Activity
Extremely selective, non-peptide NPY Y 5 receptor antagonist. Displays > 1000-fold selectivity over Y 1 , Y 2 and Y 4 receptors; IC 50 values are 1.4, 2765, 7187 and 5637 nM at cloned rat Y 5 , Y 1 , Y 2 and Y 4 receptors respectively. Potently inhibits NPY-induced food intake following i.p. administration in diabetic, free-feeding and fasted rats.
