Evidence that [Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord

Br J Pharmacol. 1998 Nov;125(5):949-51. doi: 10.1038/sj.bjp.0702188.

Abstract

[Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a pseudopeptide analogue of nociceptin is an antagonist in peripheral assays. Here, using in vivo electrophysiological recordings of dorsal horn neurones, [Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 appears to have agonist activity after spinal administration. The noxious evoked activity of the neurones was inhibited by [Phe1 psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, which was as potent as nociceptin itself.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / pharmacology*
  • Anesthesia
  • Animals
  • CHO Cells
  • Cricetinae
  • Humans
  • Male
  • Narcotic Antagonists*
  • Neurons / drug effects
  • Nociceptin
  • Nociceptin Receptor
  • Opioid Peptides / chemistry
  • Opioid Peptides / pharmacology*
  • Peptide Fragments / pharmacology*
  • Peptides / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Opioid / agonists*
  • Spinal Cord / drug effects*
  • Spinal Cord / metabolism

Substances

  • Analgesics
  • Narcotic Antagonists
  • Opioid Peptides
  • Peptide Fragments
  • Peptides
  • Receptors, Opioid
  • nociceptin (1-13)-NH2, Phe(1)-psi(CH2-NH)-Gly(2)-
  • Nociceptin Receptor