NPY1R inhibitor

Neuropeptide Y receptor type 1 (NPY1R) inhibitors, also known as NPY1R antagonists, are a class of compounds designed to block the activity of the Y1 receptor, a G protein-coupled receptor primarily activated by neuropeptide Y (NPY). NPY is one of the most abundant neuropeptides in the mammalian nervous system and plays a critical role in regulating energy homeostasis, appetite, anxiety, and vascular tone. NPY1R is widely expressed in the hypothalamus, where it mediates the orexigenic (appetite-stimulating) effects of NPY, and in the peripheral vasculature, where it contributes to vasoconstriction. Consequently, NPY1R inhibitors have been investigated as potential therapeutic agents for the treatment of obesity, metabolic disorders, anxiety, and hypertension. While several small molecule antagonists like BIBP-3226 and velneperit (S-2367) have reached clinical or advanced preclinical stages, none have yet achieved widespread regulatory approval for primary metabolic indications.

Other names

Neuropeptide Y receptor type 1 antagonistNPY Y1 receptor antagonistNPY1R antagonistNPY-1R antagonistNPY 1R antagonist