UFP-112 a potent and long-lasting agonist selective for the Nociceptin/Orphanin FQ receptor

CNS Neurosci Ther. 2011 Jun;17(3):178-98. doi: 10.1111/j.1755-5949.2009.00107.x. Epub 2010 May 18.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Drug Design
  • Humans
  • Ligands
  • Opioid Peptides / chemistry
  • Opioid Peptides / pharmacology*
  • Pain / drug therapy
  • Pain / physiopathology
  • Peptides / pharmacology
  • Receptors, Opioid / agonists*
  • Synaptic Transmission / drug effects

Substances

  • Ligands
  • Opioid Peptides
  • Peptides
  • Receptors, Opioid
  • nociceptin-amide, Nphe(1)-(pF)Phe(4)-Aib(7)-Arg(14)-Lys(15)-
  • nociceptin receptor