Ontology highlight
ABSTRACT:
SUBMITTER: Guerrini R
PROVIDER: S-EPMC2732566 | biostudies-literature | 2009 Jul
REPOSITORIES: biostudies-literature
Guerrini Remo R Camarda Valeria V Trapella Claudio C Caló Girolamo G Rizzi Anna A Ruzza Chiara C Fiorini Stella S Marzola Erika E Reinscheid Rainer K RK Regoli Domenico D Salvadori Severo S
Journal of medicinal chemistry 20090701 13
Neuropeptide S (NPS) regulates various biological functions by activating the NPS receptor (NPSR). Previous studies demonstrated that the substitution of Gly(5) with d-amino acids generates NPSR antagonists. Eleven [d-Xaa(5)]NPS derivatives were synthesized and pharmacologically tested measuring [Ca(2+)](i) in HEK293(mNPSR) cells. The results confirmed that the [d-Xaa(5)] substitution promotes antagonist activity with potency inversely related to the side chain size and allowed identification of ...[more]