The molecular and behavioral pharmacology of the orphanin FQ/nociceptin peptide and receptor family

Pharmacol Rev. 2001 Sep;53(3):381-415.


The isolation of an opioid receptor-related clone soon led to the isolation and characterization of a new neuropeptide, termed orphanin FQ or nociceptin (OFQ/N). This heptadecapeptide binds to the NOP(1) (previously termed ORL1) receptor with exceedingly high affinity, but does not interact directly with classical opioid receptors. Functionally, the actions of OFQ/N are diverse and intriguing. Most work has focused upon pain mechanisms, where OFQ/N has potent anti-analgesic actions supraspinally and analgesic actions spinally. Other OFQ/N activities are less clear. The diversity of responses might reflect NOP(1) receptor heterogeneity, but this remains to be established. The actions of this neurochemical system may also be uniquely dependent on contextual factors, both genetic and environmental. This review will address the molecular biology and behavioral pharmacology of OFQ/N and its receptor.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Cloning, Molecular
  • Humans
  • Memory / drug effects
  • Mice
  • Molecular Biology*
  • Motor Activity / drug effects
  • Opioid Peptides* / chemistry
  • Opioid Peptides* / metabolism
  • Opioid Peptides* / pharmacology
  • Pain / drug therapy*
  • Rats
  • Receptors, Opioid / metabolism*
  • Vasodilator Agents* / chemistry
  • Vasodilator Agents* / metabolism
  • Vasodilator Agents* / pharmacology


  • Opioid Peptides
  • Receptors, Opioid
  • Vasodilator Agents
  • nociceptin
  • nociceptin receptor