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

@article{Meunier1995IsolationAS,
  title={Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor},
  author={Jean Claude Meunier and Catherine Mollereau and Lawrence Toll and Charles Suaudeau and Christiane Moisand and Paul Alvinerie and J. L. Butour and Jean Claude Guillemot and Pascual Ferrara and Bernard Monsarrat and Honoré Mazarguil and Gilbert Vassart and Marc Parmentier and Jean Costentin},
  journal={Nature},
  year={1995},
  volume={377},
  pages={532-535}
}
THE ORL1 receptor, an orphan receptor whose human1and murine2á¤-8 complementary DNAs have recently been characterized, structurally resembles opioid receptors and is negatively coupled with adenylate cyclase1. 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… 
Molecular characterization and functional expression of opioid receptor-like1 receptor*
TLDR
Stimulation with ORL1 specific agonist, nociceptin/orphanin FQ, increased [35S]GTP γ S binding to SK-N-SH cell membranes, and attenuated, forskolin-stimulated accumulation of cellular cAMP, indicative that activation of OrL1 activates G proteins and inhibits adenylyl cyclase.
Structure-Activity Relationship Studies on the Novel Neuropeptide Orphanin FQ*
TLDR
Results indicate that the mode of interaction of OFQ with its receptor may be different from that of the opioid peptides with their respective receptors and might therefore account for the observed selectivity.
N-terminal modifications leading to peptide ORL1 partial agonists and antagonists.
  • A. Judd, A. Kaushanskaya, L. Toll
  • Biology, Chemistry
    The journal of peptide research : official journal of the American Peptide Society
  • 2003
TLDR
The pharmacological activity of a series of N-terminally modified hexapeptides with high affinity for ORL1 are described, found to possess modest analgesic activity, but it was unable to block the morphine modulatory activity of N/OFQ.
Endomorphin peptides: pharmacological and functional implications of these opioid peptides in the brain of mammals. Part one
TLDR
The structure-relationship activity of both endomorphin molecules comparing their binding properties to different opioid receptors are reviewed, leading several authors to suggest the potential endogenous role of these peptides in major physiological processes.
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