Open AccessUFP‐112 a Potent and Long‐Lasting Agonist Selective for the Nociceptin/Orphanin FQ Receptor
Author(s) -
Calo' Girolamo,
Rizzi Anna,
Cifani Carlo,
Di Bonaventura Maria Vittoria Micioni,
Regoli Domenico,
Massi Maurizio,
Salvadori Severo,
Lambert David G.,
Guerrini Remo
Publication year - 2011
Publication title -
cns neuroscience and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.403
H-Index - 69
eISSN - 1755-5949
pISSN - 1755-5930
DOI - 10.1111/j.1755-5949.2009.00107.x
Subject(s) - nop , nociceptin receptor , agonist , chemistry , receptor , in vivo , pharmacology , endogenous agonist , biochemistry , medicine , biology , opioid peptide , opioid , microbiology and biotechnology , dopamine receptor d1
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.