192322-50-2

CGP 71683 is an antagonist of neuropeptide Y (NPY) receptor Y₅ (IC₅₀ = 1.4 nM in a radioligand binding assay). It is selective for Y₅ over Y₁, Y₂, and Y₄ receptors (IC₅₀s = 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.

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.

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