NPY Y₅ receptor Antagonist

MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a K_i of 1.6 nM.

CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a K_i of 1.3 nM, and shows no obvious activity at Y1 receptor (K_i, >4000 nM) and Y2 receptor (K_i, 200 nM) in cell membranes.

NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a K_i of 8 nM against human Y5.

Velneperit (S-2367) is an orally active neuropeptide Y (NPY) Y5 receptor antagonist that can penetrate the blood-brain barrier. Velneperit inhibits the appetite-stimulating and metabolism-inhibiting effects mediated by NPY. Velneperit selectively improves diet-induced obesity in mice. Velneperit enhances the expression of fear acutely by removing the inhibition of CeA Drd2 neurons. Velneperit can be used for the study of obesity.

L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a K_i of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.

Lu AA33810 is a selective, orally active and brain-penetrant antagonist of neuropeptide Y5 receptor with a K_i of 1.5 nM for the rat receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects.

Neuropeptide Y5 receptor ligand-1 (compound 54), a carbazole derivative, is a potent neuropeptide Y5 (NPY-5) receptor antagonist.

GW438014A is a selective NPY-Y5 receptor competitive antagonist capable of crossing the blood-brain barrier, with IC₅₀ values of 197 nM and 211 nM against human receptors. GW438014A reverses PYY-mediated inhibition of Forskolin (HY-15371)-induced cAMP production, reduces NPY-induced food intake and nocturnal food intake in rodents, decreases body weight gain and fat mass in Zucker rats, and inhibits centrally mediated feeding behavior. GW438014A can be used in research related to obesity and epilepsy.

SCH 430765 is potent and selective NPY5 receptor antagonist. SCH 430765 can be used for the study of obesity.

J-115814 is a potent and selective neuropeptide Y1 antagonist with K_i values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors.

GW438014A free base is a selective NPY-Y5 receptor competitive antagonist capable of crossing the blood-brain barrier, with IC₅₀ values of 197 nM and 211 nM against human receptors. GW438014A free base reverses PYY-mediated inhibition of Forskolin (HY-15371)-induced cAMP production, reduces NPY-induced food intake and nocturnal food intake in rodents, decreases body weight gain and fat mass in Zucker rats, and inhibits centrally mediated feeding behavior. GW438014A free base can be used in research related to obesity and epilepsy.