Author/Authors :
Remo Guerrini، نويسنده , , Daniela Rizzi، نويسنده , , Marina Zucchini، نويسنده , , Roberto Tomatis، نويسنده , , Domenico Regoli، نويسنده , , Girolamo Caloʹ، نويسنده , , Severo Salvadori، نويسنده ,
Abstract :
The synthesis and pharmacological activity of novel nociceptin/orphanin FQ (N/OFQ) analogues modified in the Phe1-Gly2 peptide bond are reported. The aim of the present work was to elucidate the importance of this peptide bond for the N/OFQ receptor (NOP) interaction. Our study indicates that the first peptide bond in N/OFQ is important but not crucial for interaction with the N/OFQ receptor; for instance, substitution with a methyleneoxy bond generates an agonist derivative just 3-fold less potent than the reference compound.
