title: Neuropeptide S receptor: recent updates on nonpeptide antagonist discovery.
abstract: Neuropeptide S (NPS) is a 20-amino acid peptide of great interest due to its possible involvement in several biological processes, including food intake, locomotion, wakefulness, arousal, and anxiety. Structure-activity relationship studies of NPS have identified key points for structural modifications with the goal of modulating NPS receptor (NPSR) agonist activity or achieving antagonism at the same receptor. Only limited information is available for nonpeptide NPSR antagonists. In the last year, several studies have been reported in literature which present various series of small molecules as antagonists of this receptor. The results allow a comparison of the structures and activities of these molecules, leading to the design of new ligands with increased potency and improved pharmacological and pharmacokinetic profiles. This work presents a brief overview of the available information regarding structural features and pharmacological characterization of published nonpeptide NPSR antagonists.
authors: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino via S. Agostino 1, 62032 Camerino, MC, Italy. diego.dalben@unicam.it
authors: Diego
authors: D
authors: Dal Ben
authors: Ippolito
authors: I
authors: Antonini
authors: Michela
authors: M
authors: Buccioni
authors: Catia
authors: C
authors: Lambertucci
authors: Gabriella
authors: G
authors: Marucci
authors: Ajiroghene
authors: A
authors: Thomas
authors: Rosaria
authors: R
authors: Volpini
authors: Gloria
authors: G
authors: Cristalli
mesh_terms: D002118:Calcium / Q000378:metabolism; D000242:Cyclic AMP / Q000378:metabolism; D005663:Furans / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D009479:Neuropeptides / Q000737:chemistry; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D005663:Furans; D007093:Imidazoles; C484532:NPSR1 protein, human; D009479:Neuropeptides; D011743:Pyrimidines; D015363:Quinolones; D043562:Receptors, G-Protein-Coupled; C506531:neuropeptide S, human; C029899:imidazole; D000242:Cyclic AMP; C030986:pyrimidine; D002118:Calcium; C039281:furan