[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 is an agonist of the nociceptin (ORL1) receptor

Eur J Pharmacol. 1998 May 15;349(1):R5-6. doi: 10.1016/s0014-2999(98)00273-8.

Abstract

[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a pseudopeptide analog of nociceptin, has been shown to be a selective 'antagonist' of the nociceptin receptor in the isolated guinea pig ileum and mouse vas deferens preparations (Guerrini et al., 1998. Br. J. Pharmacol. 123, 163-165). However, in recombinant chinese hamster ovary cells expressing the human nociceptin receptor, we find that the pseudopeptide is a potent (IC50 = 7.5 nM) and fully efficacious inhibitor of forskolin-induced accumulation of cAMP, thus behaving as a pure 'agonist' rather than an antagonist of the receptor. The contrary behaviour of the pseudopeptide in smooth muscle and transformed cells may suggest that different nociceptin receptor types are being addressed in the two systems.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cell Line, Transformed
  • Colforsin / pharmacology
  • Cricetinae
  • Cyclic AMP / metabolism
  • Humans
  • Nociceptin
  • Nociceptin Receptor
  • Opioid Peptides / metabolism
  • Opioid Peptides / pharmacology*
  • Peptide Fragments / metabolism
  • Peptide Fragments / pharmacology*
  • Receptors, Opioid / agonists*
  • Receptors, Opioid / biosynthesis
  • Receptors, Opioid / metabolism

Substances

  • Opioid Peptides
  • Peptide Fragments
  • Receptors, Opioid
  • nociceptin (1-13)-NH2, Phe(1)-psi(CH2-NH)-Gly(2)-
  • Colforsin
  • Cyclic AMP
  • Nociceptin Receptor