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  • Further Studies at Neuropep...
    Guerrini, Remo; Camarda, Valeria; Trapella, Claudio; Caló, Girolamo; Rizzi, Anna; Ruzza, Chiara; Fiorini, Stella; Marzola, Erika; Reinscheid, Rainer K; Regoli, Domenico; Salvadori, Severo

    Journal of medicinal chemistry, 07/2009, Letnik: 52, Številka: 13
    Journal Article

    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-Xaa5NPS 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 t Bu-d-Gly5NPS.