Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor

@article{Reinscheid1995OrphaninFA,
  title={Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor},
  author={Rainer K Reinscheid and H. P. Nothacker and Anne Bourson and Ali Ardati and Robert A. Henningsen and James R. Bunzow and David K. Grandy and Hanno Langen and Frederick J. Monsma and Olivier Civelli},
  journal={Science},
  year={1995},
  volume={270},
  pages={792 - 794}
}
A heptadecapeptide was identified and purified from porcine brain tissue as a ligand for an orphan heterotrimeric GTP- binding protein (G protein)- coupled receptor (LC132) that is similar in sequence to opioid receptors. This peptide, orphanin FQ, has a primary structure reminiscent of that of opioid peptides. Nanomolar concentrations of orphanin FQ inhibited forskolin-stimulated adenylyl cyclase activity in cells transfected with LC132. This inhibitory activity was not affected by the… 
Orphanin FQ is a functional anti-opioid peptide
TLDR
It is proposed that orphanin FQ is a functional anti-opioid peptide that reverses opioid-mediated (i.e. naloxone-sensitive) stress-induced antinociception in three different algesiometric assays.
Nociceptin/Orphanin FQ: Actions within the Brain
  • S. Meis
  • Chemistry, Medicine
    The Neuroscientist : a review journal bringing neurobiology, neurology and psychiatry
  • 2003
TLDR
Systemic application of N/OFQ elicits a unique range of responses, including a wide range of effects on pain processing such as hyperalgesia, analgesia, and allodynia, as well as anxiolytic actions, modulation of opioid-mediated processes, and influences on learning and memory.
Structure-activity studies on nociceptin/orphanin FQ: from full agonist, to partial agonist, to pure antagonist.
TLDR
The new peptide, nociceptin (NC), has a primary sequence recalling that of opioid peptides and has been shown to act mainly as an antagonist outside the brain and as an agonist in the central nervous system.
Structure of the Nociceptin/Orphanin FQ Receptor in Complex with a Peptide Mimetic
TLDR
The crystal structure of human NOP is reported, solved in complex with the peptide mimetic antagonist compound-24 (C-24), revealing atomic details of ligand–receptor recognition and selectivity and providing a new structural template for the design of NOP ligands.
Inhibitory actions of nociceptin (orphanin FQ) on rat supraoptic nucleus oxytocin and vasopressin neurones in vitro.
TLDR
The nociceptin gene is expressed in the SON7, and because previous studies have shown inhibitory actions of opioids within the SONS on both oxytocin and vasopressin neurones, it is investigated whether nocICEptin could act to oppose opioids on SON neurones.
Orphanin FQ/nociceptin: an endogenous peptide agonist for the orphan opioid receptor.
TLDR
A new development in opioid pharmacology is summarized—isolation of a novel receptor involved in pain processing and discovery of an endogenous ligand for this receptor.
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.
Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor.
  • J. Meunier
  • Medicine, Chemistry
    European journal of pharmacology
  • 1997
TLDR
The discovery of noc/oFQ, a neuropeptide with multiple functions, will certainly improve the knowledge of brain physiology, and may find therapeutic applications, for example in the management of pain or hyponatremic and water-retaining diseases.
Biochemical evidence for orphanin FQ/nociceptin receptor heterogeneity in mouse brain.
TLDR
Competition studies confirm the high affinity of OFQ/N for this site, but shallow Hill slopes suggest heterogeneity, and studies suggest the presence of heterogeneous, functionally active OFZ/N receptors in mouse brain.
Nociceptin/orphanin FQ metabolism and bioactive metabolites
The endogenous ligand for the orphan NOR receptor (earlier named ORL1) was recently discovered. This ligand, nociceptin/orphanin FQ is involved in a number of pharmacological actions in the CNS,
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