gr-231118

Potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses

GR231118 TFA, a neuropeptide Y C-terminus analogue, acts as a potent, competitive, and relatively selective antagonist at the human neuropeptide YY receptor, exhibiting a pKi of 10.4. It serves as a strong agonist at the human neuropeptide YY4 receptor with a pEC50 of 8.6 and a pKi of 9.6, while demonstrating weak agonistic activity at both human and rat neuropeptide YY2 and YY5 receptors. Additionally, this compound shows high affinity for the mouse neuropeptide YY6 receptor, with a pKi value of 8.8 [1].