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.

Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.

GUERRINI, Remo
Primo
;
CAMARDA, Valeria
Secondo
;
TRAPELLA, Claudio;CALO', Girolamo;RIZZI, Anna;RUZZA, Chiara;FIORINI, Stella;MARZOLA, Erika;REGOLI, Domenico;SALVADORI, Severo
Ultimo
2009

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.
2009
Guerrini, Remo; Camarda, Valeria; Trapella, Claudio; Calo', Girolamo; Rizzi, Anna; Ruzza, Chiara; Fiorini, Stella; Marzola, Erika; Reinscheid, Rk; Reg...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/536230
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