Agonistic effects of the opioid buprenorphine on the nociceptin/OFQ receptor

Peptides. 2000 Jul;21(7):1141-6. doi: 10.1016/s0196-9781(00)00252-7.


The nociceptin/orphanin FQ (N/OFQ) receptor (e.g. the human ortholog ORL1) has been shown to be pharmacologically distinct from classic opioid receptors. Recently, we have identified buprenorphine as a full ORL1 agonist using a reporter gene assay. For further functional analysis, buprenorphine's effects on ORL1 receptors were investigated using a K(+) channel (GIRK1) assay in Xenopus oocytes and GTPgammaS assay in CHO-K1 membrane preparations. In both assays, buprenorphine behaved as a partial agonist compared to nociceptin itself. The N/OFQ agonism of buprenorphine might contribute to actions of buprenorphine in pain models in vivo beside its mu- or kappa-opioid receptor mediated effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics, Opioid / pharmacology
  • Animals
  • Barium Compounds / pharmacology
  • Buprenorphine / pharmacology*
  • CHO Cells
  • Chlorides / pharmacology
  • Cricetinae
  • Dose-Response Relationship, Drug
  • Genes, Reporter
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Naloxone / pharmacology
  • Narcotic Antagonists / pharmacology
  • Oocytes / drug effects
  • Patch-Clamp Techniques
  • Potassium Channels / drug effects
  • Protein Binding
  • Receptors, Opioid / agonists*
  • Receptors, Opioid / metabolism
  • Xenopus


  • Analgesics, Opioid
  • Barium Compounds
  • Chlorides
  • Narcotic Antagonists
  • Potassium Channels
  • Receptors, Opioid
  • barium chloride
  • Naloxone
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Buprenorphine
  • nociceptin receptor