Antinociceptive potency of enkephalins and enkephalinase inhibitors in the mouse model of colorectal distension-proof-of-concept

Adam Fabisiak , Małgorzata Sobocińska , Elżbieta Kamysz , Jakub Fichna , Marta Zielińska


Irritable bowel syndrome (IBS) is a chronic disease characterized by abdominal pain and changes in bowel habits. Patients with IBS comprise a significant portion of attendants at the outpatient clinics. Targeting intestinal opioid receptors was found successful in alleviating pain and diarrhea - two major symptoms of IBS. In this study, we aimed to evaluate a novel potential pharmacological option: the use of enkephalinase inhibitors in therapy of visceral pain occurring in the course of IBS. We thus assessed the antinociceptive efficacy of enkephalins: Leu-enkephalin and Met-enkephalin, and enkephalinase inhibitors: opiorphin and sialorphin in the mouse model of visceral pain induced by colorectal distension. Leu-enkephalin, Met-enkephalin, and sialorphin, but not opiorphin, at the dose of 1 mg/kg injected subcutaneously potently decreased the visceromotor response to colon distension as compared to control. To conclude, enkephalinase inhibitors are worth being considered as potential therapeutics in patients with chronic abdominal pain and/or changed bowel habits, that is, suffering from IBS.
Author Adam Fabisiak
Adam Fabisiak,,
, Małgorzata Sobocińska (FCh / DMBt / LChBM)
Małgorzata Sobocińska,,
- Laboratory of Chemistry of Biological Macromolecules
, Elżbieta Kamysz (FCh / DMBt / LChBM)
Elżbieta Kamysz,,
- Laboratory of Chemistry of Biological Macromolecules
, Jakub Fichna
Jakub Fichna,,
, Marta Zielińska
Marta Zielińska,,
Journal seriesChemical Biology & Drug Design, ISSN 1747-0277, e-ISSN 1747-0285, (A 25 pkt)
Issue year2018
Publication size in sheets0.5
Keywords in Englishabdominal pain, colorectal distension, hypersensitivity, irritable bowel syndrome, visceral pain
ASJC Classification1313 Molecular Medicine; 1303 Biochemistry
Languageen angielski
Score (nominal)25
Score sourcejournalList
ScoreMinisterial score = 25.0, 28-01-2020, ArticleFromJournal
Publication indicators WoS Citations = 2; Scopus SNIP (Source Normalised Impact per Paper): 2018 = 0.708; WoS Impact Factor: 2018 = 2.256 (2) - 2018=2.434 (5)
Citation count*3 (2020-05-21)
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* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or Perish system.
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