| Literature DB >> 19473027 |
Remo Guerrini1, Valeria Camarda, Claudio Trapella, Girolamo Caló, Anna Rizzi, Chiara Ruzza, Stella Fiorini, Erika Marzola, Rainer K Reinscheid, Domenico Regoli, Severo Salvadori.
Abstract
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 the novel potent NPSR peptide antagonist [(t)Bu-d-Gly(5)]NPS.Entities:
Mesh:
Substances:
Year: 2009 PMID: 19473027 PMCID: PMC2732566 DOI: 10.1021/jm900604g
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446