Further Studies at Neuropeptide S Position 5: Discovery of Novel Neuropeptide S Receptor Antagonists
journal contributionposted on 09.07.2009 by Remo Guerrini, Valeria Camarda, Claudio Trapella, Girolamo Caló, Anna Rizzi, Chiara Ruzza, Stella Fiorini, Erika Marzola, Rainer K. Reinscheid, Domenico Regoli, Severo Salvadori
Any type of content formally published in an academic journal, usually following a peer-review process.
Neuropeptide S (NPS) regulates various biological functions by activating the NPS receptor (NPSR). Previous studies demonstrated that the substitution of Gly5 with d-amino acids generates NPSR antagonists. Eleven [d-Xaa5]NPS derivatives were synthesized and pharmacologically tested measuring [Ca2+]i in HEK293mNPSR cells. The results confirmed that the [d-Xaa5] substitution promotes antagonist activity with potency inversely related to the side chain size and allowed identification of the novel potent NPSR peptide antagonist [tBu-d-Gly5]NPS.