NOP receptor mediates anti-analgesia induced by agonist–antagonist opioids

Highlights • In male rats, κ-opioids produce analgesia, followed by anti-analgesia. • Low-dose naloxone blocked anti-analgesia but not analgesia. • Nociceptin/orphanin FQ (NOP) antagonists also blocked anti-analgesia. • Selective kappa antagonist nor-BNI did not block nalbuphine-induced anti-analges...

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Bibliographic Details
Published in:Neuroscience 2014-01, Vol.257, p.139-148
Main Authors: Gear, R.W, Bogen, O, Ferrari, L.F, Green, P.G, Levine, J.D
Format: Article
Language:English
Subjects:
Analgesics - pharmacology
Analysis of Variance
Animals
Benzeneacetamides
Biological and medical sciences
Dose-Response Relationship, Drug
Drug Interactions
Female
Fundamental and applied biological sciences. Psychology
Male
Nalbuphine - pharmacology
Naloxone - pharmacology
Narcotic Antagonists - pharmacology
Neurology
Nociceptin
Opioid Peptides - metabolism
Pain Measurement - drug effects
Pain Threshold - drug effects
Protein Binding - drug effects
Pyrrolidines
Rats
Rats, Sprague-Dawley
Sex Differentiation
Vertebrates: nervous system and sense organs
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Summary:Highlights • In male rats, κ-opioids produce analgesia, followed by anti-analgesia. • Low-dose naloxone blocked anti-analgesia but not analgesia. • Nociceptin/orphanin FQ (NOP) antagonists also blocked anti-analgesia. • Selective kappa antagonist nor-BNI did not block nalbuphine-induced anti-analgesia. • Clinically used agonist–antagonists act at NOP receptors to produce anti-analgesia.
ISSN:0306-4522
1873-7544
DOI:10.1016/j.neuroscience.2013.10.061