10.1021/jm900604g.s001
Remo Guerrini
Remo
Guerrini
Valeria Camarda
Valeria
Camarda
Claudio Trapella
Claudio
Trapella
Girolamo Caló
Girolamo
Caló
Anna Rizzi
Anna
Rizzi
Chiara Ruzza
Chiara
Ruzza
Stella Fiorini
Stella
Fiorini
Erika Marzola
Erika
Marzola
Rainer K. Reinscheid
Rainer K.
Reinscheid
Domenico Regoli
Domenico
Regoli
Severo Salvadori
Severo
Salvadori
Further Studies at Neuropeptide S Position 5: Discovery of Novel Neuropeptide S Receptor Antagonists
American Chemical Society
2009
side chain size
Novel Neuropeptide S Receptor AntagonistsNeuropeptide S
NPSR peptide antagonist
NPS receptor
Previous studies
Gly 5
HEK 293mNPSR cells
substitution
antagonist activity
NPSR antagonists
2009-07-09 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Further_Studies_at_Neuropeptide_S_Position_5_Discovery_of_Novel_Neuropeptide_S_Receptor_Antagonists/2844406
Neuropeptide S (NPS) regulates various biological functions by activating the NPS receptor (NPSR). Previous studies demonstrated that the substitution of Gly<sup>5</sup> with d-amino acids generates NPSR antagonists. Eleven [d-Xaa<sup>5</sup>]NPS derivatives were synthesized and pharmacologically tested measuring [Ca<sup>2+</sup>]<sub>i</sub> in HEK293<sub>mNPSR</sub> cells. The results confirmed that the [d-Xaa<sup>5</sup>] substitution promotes antagonist activity with potency inversely related to the side chain size and allowed identification of the novel potent NPSR peptide antagonist [<sup><i>t</i></sup>Bu-d-Gly<sup>5</sup>]NPS.