Isolation and structure of the endogenous agonist of opioid receptor- like ORL1 receptor

  • Meunier J
  • Mollereau C
  • Toll L
 et al. 
  • 2


    Mendeley users who have this article in their library.
  • N/A


    Citations of this article.


The ORL1 receptor, an orphan receptor whose human and murine complementary DNAs have recently been characterized, structurally resembles opioid receptors and is negatively coupled with adenylate cyclase. ORL1 transcripts are particularly abundant in the central nervous system. Here we report the isolation, on the basis of its ability to inhibit the cyclase in a stable recombinant CHO(ORL1+) cell line, of a neuropeptide that resembles dynorphin A9 and whose amino acid sequence is Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys- Leu-Ala-Asn-Gln. The rat-brain cDNA encodes the peptide flanked by Lys- Arg proteolytic cleavage motifs. The synthetic heptadecapeptide potently inhibits adenylate cyclase in CHO(ORL1+) cells in culture and induces hyperalgesia when administered intracerebroventricularly to mice. Taken together, these data indicate that the newly discovered heptadecapeptide is an endogenous agonist of the ORL1 receptor and that it may be endowed with pro-nociceptive properties.

Author-supplied keywords

  • Amino Acid Sequence
  • Animal
  • Base Sequence
  • CHO Cells
  • DNA, Antisense/pharmacology
  • DNA, Complementary
  • Dynorphins/chemistry
  • Hamsters
  • Human
  • Molecular Sequence Data
  • Opioid Peptides/chemistry/*isolation & purificatio
  • Rats
  • Receptors, Opioid/*agonists
  • Support, Non-U.S. Gov't
  • Support, U.S. Gov't, P.H.S.

Get free article suggestions today

Mendeley saves you time finding and organizing research

Sign up here
Already have an account ?Sign in

Find this document

There are no full text links


  • J C Meunier

  • C Mollereau

  • L Toll

  • C Suaudeau

  • C Moisand

  • P Alvinerie

Cite this document

Choose a citation style from the tabs below

Save time finding and organizing research with Mendeley

Sign up for free