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Nociceptin/Orphanin FQ(1-13)NH2 analogues modified in the Phe1-Gly2 peptide bond
Remo Guerrini1, Daniela Rizzi, Marina Zucchini
1Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, via Fossato di Mortara, 17/19, 44100 Ferrara, Italy. r.guerrini@unife.it
Abstract:
The synthesis and pharmacological activity of novel nociceptin/orphanin FQ (N/OFQ) analogues modified in the Phe(1)-Gly(2) 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.
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