Inhibition of experimental visceral pain in rodents by cebranopadol

Klaus Schiene, Wolfgang Schröder, Klaus Linz, Stefanie Frosch, Thomas M. Tzschentke, Thomas Christoph, Jennifer Y. Xie, Frank Porreca

Research output: Contribution to journalArticlepeer-review

5 Scopus citations


The aim of this study was to investigate the efficacy of cebranopadol in two rodent models of visceral pain. Cebranopadol is a first-in-class analgesic with agonist activity at the nociceptin/orphanin FQ opioid peptide receptor and classical μ-, δ- and κ-opioid peptide receptors. Colitis was induced in Naval Medical Research Institute mice by intra-rectal infusion of mustard oil. The effects of intravenous cebranopadol pretreatment on spontaneous pain behaviours and referred allodynia and hyperalgesia were assessed. Pancreatitis was induced in Sprague-Dawley rats by intravenous administration of dibutyltin dichloride. After 6 days, the effects of intravenous cebranopadol on withdrawal reactions to mechanical abdominal stimulation with von Frey filaments were assessed. In mice with experimental colitis, cebranopadol dose-dependently inhibited spontaneous pain behaviours and allodynic and hyperalgesic withdrawal reactions, with half-maximal effective dose values of 4.6 μg/kg [95% confidence interval (CI): 2.9-7.9] for inhibition of spontaneous pain behaviours, 2.2 μg/kg (95% CI: 1.3-3.4) for inhibition of referred allodynia and 2.4 μg/kg (95% CI: 1.4-3.6) for inhibition of referred hyperalgesia in mice with colitis. In rats with experimental pancreatitis, cebranopadol dose-dependently inhibited abdominal tactile allodynia (half-maximal effective dose, 0.13 μg/kg; 95% CI: 0.03-0.49). Behavioural manifestations of visceral pain were almost completely abolished at the highest doses tested in mice (17.2 μg/kg, intravenous) and rats (2.4 μg/kg, intravenous). We conclude that cebranopadol is a potent and effective antiallodynic and antihyperalgesic agent in rodent models of visceral pain.

Original languageEnglish (US)
Pages (from-to)320-326
Number of pages7
JournalBehavioural Pharmacology
Issue number4
StatePublished - Jun 1 2019


  • allodynia
  • analgesia
  • cebranopadol
  • hyperalgesia
  • mouse
  • nociceptin/orphanin FQ opioid peptide receptor
  • opioid peptide receptor
  • rat
  • visceral pain

ASJC Scopus subject areas

  • Pharmacology
  • Psychiatry and Mental health


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