UFP-112 a Potent and Long-Lasting Agonist Selective for the Nociceptin/Orphanin FQ Receptor

Autor: Maurizio Massi, Severo Salvadori, Remo Guerrini, Girolamo Calo, Maria Vittoria Micioni Di Bonaventura, David G. Lambert, Carlo Cifani, Domenico Regoli, Anna Rizzi
Rok vydání: 2010
Předmět:
Zdroj: CNS Neuroscience & Therapeutics. 17:178-198
ISSN: 1755-5930
DOI: 10.1111/j.1755-5949.2009.00107.x
Popis: Nociceptin/orphanin FQ (N/OFQ) controls several biological functions via selective activation of the N/OFQ peptide receptor (NOP). [(pF)Phe(4) Aib(7) Arg(14) Lys(15) ]N/OFQ-NH(2) (UFP-112) is an NOP receptor ligand designed using a combination of several chemical modifications in the same peptide sequence that increase NOP receptor affinity/potency and/or reduce susceptibility to enzymatic degradation. In the present review article, we summarize data from the literature and present original findings on the in vitro and in vivo pharmacological features of UFP-112. Moreover, important biological actions and possible therapeutic indications of NOP receptor agonists are discussed based on the results obtained with UFP-112 and compared with other peptide and nonpeptide NOP receptor ligands.
Databáze: OpenAIRE