Neuropeptide Y receptor (NPYR) (NPYR)

Neuropeptide Y (NPY) is a 36-amino acid peptide and one of the most abundant neurotransmitters in the mammalian central and peripheral nervous systems [2, 5, 6]. It belongs to the pancreatic polypeptide family and exerts its biological effects through a group of G protein-coupled receptors, primarily the Y1, Y2, Y4, and Y5 subtypes [2, 4, 6, 8]. The NPY system plays a critical role in regulating appetite and energy homeostasis, where NPY acts as a potent orexigenic (appetite-stimulating) signal in the hypothalamus [1, 5, 7, 9]. Beyond metabolism, NPY is involved in modulating anxiety, stress responses, circadian rhythms, and cardiovascular function [2, 4, 5, 6]. In the context of drug development, NPY receptors are significant therapeutic targets for obesity, type 2 diabetes, and metabolic syndrome [6, 7, 8, 9]. Antagonists of the Y1 and Y5 receptors have been extensively studied for their potential to suppress food intake, while Y2 receptor agonists are explored for their ability to inhibit NPY release via presynaptic feedback [1, 4, 6, 7]. Additionally, the NPY system is investigated for its roles in neuroprotection, epilepsy, and cancer progression [3, 6, 10, 12]. Despite significant research, the development of clinical therapeutics has faced challenges such as low oral bioavailability, poor brain penetration, and off-target effects related to the widespread distribution of NPY receptors [1, 4, 7, 8]. Note: The input 'Neuropeptide Y neuron' refers to a cell type rather than a specific molecular target; the information provided here pertains to the NPY receptor system which is the actual therapeutic target.

Other names

NPY receptorsY receptorsNeuropeptide Y receptor family

Antagonism of Y1 or Y5 receptors to suppress appetite; Agonism of Y2 receptors to inhibit presynaptic NPY release; Modulation of Y1/Y2 receptors for anxiolytic or neuroprotective effects.