| Literature DB >> 12565930 |
Remo Guerrini1, Daniela Rizzi, Marina Zucchini, Roberto Tomatis, Domenico Regoli, Girolamo Calo', Severo Salvadori.
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.Entities:
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Year: 2003 PMID： 12565930 DOI： 10.1016/s0960-894x(02)01004-1
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823