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Neuropeptide S receptor 1 (NPSR1) is a G protein-coupled receptor that binds neuropeptide S (NPS) and mediates signal transduction in multiple tissues, notably the central nervous system and respiratory epithelium[1][3][4]. NPSR1 plays roles in the regulation of arousal, anxiety, memory, gastrointestinal function, and immune responses[1][4]. Genetic variants in NPSR1 have been strongly linked to asthma susceptibility, certain neuropsychiatric traits, and rare sleep phenotypes[1][2][3]. It is considered a therapeutic target of interest in respiratory, neuropsychiatric, and immune-mediated diseases, with several synthetic antagonists developed for experimental purposes but no drugs yet approved for clinical use[4]. Safety and patient selection considerations include genetic heterogeneity and the multifaceted roles of NPSR1 in physiology and disease.
Competitive antagonism of neuropeptide S binding to the receptor\nInhibition or enhancement of downstream G protein-coupled signaling (e.g., mobilization of intracellular Ca2+ stores, ERK phosphorylation)\nModulation of ligand-induced physiological effects (arousal, memory, anxiolysis, etc.)
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