An insurmountable NPY Y5 receptor antagonist exhibits superior anti-obesity effects in high-fat diet-induced obese mice

Neuropeptide Y (NPY) Y5 receptor plays a key role in the effects of NPY, an important neurotransmitter in the control of energy homeostasis including stimulation of food intake and inhibition of energy expenditure. The NPY-Y5 receptor system has been an attractive drug target for potential use in treating obesity. Here we report the discovery and characterization of two novel Y5 receptor antagonists, S-2367 and S-234462. Both compounds displayed high affinity for the Y5 receptor in the radio-ligand binding assay, while in the cell-based functional assay, S-2367 and S-234462 showed, respectively, surmountable and insurmountable antagonism.

Source: Neuropeptides - May 17, 2018 Category: Neuroscience Authors: Yumiko Fukasaka, Hirohide Nambu, Hideki Tanioka, Atsushi Obata, Misato Tonomura, Takayuki Okuno, Hideo Yukioka Source Type: research