The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential

@article{Lambert2008TheNF,
  title={The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential},
  author={David G Lambert},
  journal={Nature Reviews Drug Discovery},
  year={2008},
  volume={7},
  pages={694-710}
}
  • D. Lambert
  • Published 1 August 2008
  • Medicine
  • Nature Reviews Drug Discovery
Identification of the enigmatic nociceptin/orphanin FQ peptide (N/OFQ) in 1995 represented the first successful use of reverse pharmacology and led to deorphanization of the N/OFQ receptor (NOP). Subsequently, the N/OFQ–NOP system has been implicated in a wide range of biological functions, including pain, drug abuse, cardiovascular control and immunity. Although this could be considered a hurdle for the development of pharmaceuticals selective for a specific disease indication, NOP represents… 
Potential of Nociceptin/Orphanin FQ Peptide Analogs for Drug Development
TLDR
The structure of potent peptide‐based agonists, antagonists, biased analogs and bivalent ligands that target NOP receptor are reviewed to fully understand the role of NOP‐N/OFQ system in the body and may lead to designing novel therapeutics.
The endogenous nociceptin/orphanin FQ‐NOP receptor system as a potential therapeutic target for intestinal disorders
  • S. Agostini, C. Petrella
  • Medicine
    Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society
  • 2014
TLDR
Experimental and clinical studies focusing on the N/OFQergic system as pharmacological target for the therapeutic treatment of intestinal pathologies such as IBS and IBD are given.
Nociceptin/Orphanin FQ (N/OFQ) conjugated to ATTO594: a novel fluorescent probe for the N/OFQ (NOP) receptor
TLDR
A red fluorophore‐ATTO594 is conjugated to the peptide ligand N/OFQ for the NOP receptor and Nop receptor function at high (in recombinant systems) and low (on immune cells) expression is explored.
Nociceptin/orphanin FQ (N/OFQ) modulates immunopathology and airway hyperresponsiveness representing a novel target for the treatment of asthma
TLDR
The expression and function of N/OFQ and the NOP receptor were examined in healthy and asthmatic human airway tissues and the concept was further addressed in an animal model of allergic asthma.
Spinal antinociceptive effects of the novel NOP receptor agonist PWT2‐nociceptin/orphanin FQ in mice and monkeys
TLDR
The aim of the present study was to investigate the spinal effects of PWT2‐N/OFQ in nociceptive and neuropathic pain models in mice and non‐human primates.
Nociceptin/orphanin-FQ modulation of learning and memory.
TLDR
The findings supporting the role played by N/OFQ and NOP receptors in learning and memory are outlined and the underlying mechanisms are discussed.
Nociceptin Orphanin FQ 1-13 -NH 2
Nociceptin/orphanin FQ(1–13) amide is the smallest fragment of nociceptin/orphanin FQ (N/OFQ) that binds to and activates its cognate receptor, ORL1 ( Calo et al ., 1996  ; Dooley and Houghten, 1996
Nociceptin/orphanin FQ receptor antagonists as innovative antidepressant drugs.
TLDR
Clinical findings showed that plasma N/OFQ levels were significantly altered in major and post-partum depression, and bipolar disease patients, and chronic administration of a NOP antagonist restored these alterations.
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1–13)-NH2
TLDR
The results demonstrate that lipidation of N/OFQ(1–13)-NH2 is a useful strategy for obtaining G protein biased agonists for the NOP receptor.
The Nociceptin/Orphanin FQ System and the Regulation of Memory.
  • L. Moulédous
  • Chemistry, Medicine
    Handbook of experimental pharmacology
  • 2018
TLDR
The consequences of the pharmacological manipulation of the N/OFQ system by NOP receptor ligands on learning processes and on the consolidation of various types of long-term memory are described.
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References

SHOWING 1-10 OF 267 REFERENCES
Neurohumoral effects of orphanin FQ/nociceptin: relevance to cardiovascular and renal function
TLDR
This review will focus on the neural and humoral effects of OFQ/N and how this peptide may participate in the regulation of cardiovascular and renal function.
Orphanin FQ/nociceptin: a novel neuromodulator of gastrointestinal function?
TLDR
Orphanin FQ/nociceptin acts as a neuromodulator of gastrointestinal motility and may have additional roles in regulation of intestinal blood flow, active ion transport, and immunity.
Nociceptin/orphanin FQ and drugs of abuse
TLDR
Findings suggest that drugs directed at central NC receptors may represent an interesting approach to the treatment of ethanol and opiate abuse.
Nociceptin/Orphanin FQ and Its Receptor—Potential Targets for Pain Therapy?
  • H. Zeilhofer, G. Calo
  • Chemistry, Medicine
    Journal of Pharmacology and Experimental Therapeutics
  • 2003
TLDR
New insights are generated into the role of N/OFQ in pain processing and the recent development of specific antagonists at the NOP receptor and of N /OFQ precursor knock-out mice have generated new insights.
UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor.
TLDR
The analysis of the available data demonstrates that UFP-101 is a useful pharmacological tool for the investigation of the central and peripheral biological functions regulated by the N/OFQ-NOP receptor system and for defining the therapeutic potential of NOP receptor ligands.
Role of Nociceptin/Orphanin FQ in the Physiologic and Pathologic Control of the Cerebral Circulation 1s
  • W. Armstead
  • Medicine
    Experimental biology and medicine
  • 2002
TLDR
The contribution of nociceptin/orphanin FQ to impaired cerebral hemodynamics after cerebral hypoxia/ischemia and traumatic brain injury is discussed.
The molecular and behavioral pharmacology of the orphanin FQ/nociceptin peptide and receptor family.
The isolation of an opioid receptor-related clone soon led to the isolation and characterization of a new neuropeptide, termed orphanin FQ or nociceptin (OFQ/N). This heptadecapeptide binds to the
Nociceptin/orphanin FQ modulates human T cell function in vitro
TLDR
It is suggested that N/OFQ could exert a key modulatory role in human T cell functions and that some of these effects are partly prostaglandin-dependent and that N-OFQ induces prostaglandsin synthesis.
Peripheral orphanin FQ/nociceptin analgesia in the mouse.
TLDR
Antisense mapping both compounds against the murine orphan opioid receptor (KOR-3) confirmed the importance of this clone in their actions and significantly lowered the analgesic effects of both compounds.
Spinal analgesic activity of orphanin FQ/nociceptin and its fragments
TLDR
Antisense probes targeting the second and third coding exons, but not the first exon, of the cloned mouse OFQ/nociceptin receptor (KOR-3) partially block OfQ/N analgesia.
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