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British Journal of Anaesthesia 2004 93(5):626-628; doi:10.1093/bja/aeh226
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© The Board of Management and Trustees of the British Journal of Anaesthesia 2004

Editorial III: Nociceptin/orphanin FQ peptide-receptor system: are we any nearer the clinic?

T. A. Barnes and D. G. Lambert*,{dagger}

University Department of Cardiovascular Sciences (Pharmacology and Therapeutics Group), Division of Anaesthesia, Critical Care and Pain Management, Leicester Royal Infirmary, Leicester LE1 5WW, UK

* Corresponding author. E-mail: DGL3@leicester.ac.uk

The first 10% of the full text of this article appears below.

Nociceptin/orphanin FQ (N/OFQ) is a 17 amino acid peptide with activity at the nociceptin receptor (NOP), a G-protein coupled receptor related to but distinct from the opioid receptors.1 2 The functional role of this receptor, in common with classical opioid receptors (MOP-µ/DOP-{delta}/KOP-{kappa}), is to affect the transmission of nerve signals, in particular those conveying nociceptive information. This is achieved by modulating voltage-gated Ca2+ channels, K+ channels, and adenylyl cyclase via an inhibitory G-protein (Gi).1 2 The full role of the N/OFQ-NOP system remains unclear, as it has actions implicated in both the suppression and enhancement of pain. This is seemingly dependent upon the anatomical site of the receptor in that anti-opioid effects/hyperalgesia are seen supraspinally and analgesia spinally.3

Since formal identification of N/OFQ, there have been major advances in the design and evaluation of novel NOP ligands. Indeed, high potency/high efficacy agonists and high . . . [Full Text of this Article]


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