Abstract
Diarrhea-predominant irritable bowel syndrome (IBS-D) is a frequent functional disorder of the gastrointestinal (GI) tract affecting nearly one fifth of the worldwide population. IBS-D is associated with numerous symptoms including diarrhea, bloating, abdominal pain and discomfort, which significantly reduce patients’ quality of life. Due to a complex and unclear pathogenesis, effective therapy against IBS-D has not been developed yet. Nowadays, treatment is focused on non-pharmacological (e.g. changes in diet and life style) and pharmacological (e.g. loperamide, ramosetron, rifaximin) approaches. The endogenous opioid system is responsible for the maintenance of homeostasis in the GI tract. Activation of the intestinal opioid receptors (ORs), in particular μ (MOP) and δ (DOP) results in reduction of epithelial secretion and increase of water/electrolyte absorption; moreover, opioids are strong analgesic agents. Thus, ligands of ORs are a promising target in IBS-D treatment. In this review, we discuss the role of ORs in the pathogenesis of IBS-D and the use of “classical” and novel, such as P-317, eluxadoline and biphalin MOP and DOP receptor ligands in preclinical and clinical trials.
Keywords: Diarrhea, irritable bowel syndrome, MOP/DOP receptor ligands, opioid receptors, opioids.
Mini-Reviews in Medicinal Chemistry
Title:Review: The Role of MOP and DOP Receptors in Treatment of Diarrheapredominant Irritable Bowel Syndrome
Volume: 16 Issue: 18
Author(s): Agata Jarmuż, Marta Zielińska, Karolina Leń, Martyna Banaszek, Martin Storr and Jakub Fichna
Affiliation:
Keywords: Diarrhea, irritable bowel syndrome, MOP/DOP receptor ligands, opioid receptors, opioids.
Abstract: Diarrhea-predominant irritable bowel syndrome (IBS-D) is a frequent functional disorder of the gastrointestinal (GI) tract affecting nearly one fifth of the worldwide population. IBS-D is associated with numerous symptoms including diarrhea, bloating, abdominal pain and discomfort, which significantly reduce patients’ quality of life. Due to a complex and unclear pathogenesis, effective therapy against IBS-D has not been developed yet. Nowadays, treatment is focused on non-pharmacological (e.g. changes in diet and life style) and pharmacological (e.g. loperamide, ramosetron, rifaximin) approaches. The endogenous opioid system is responsible for the maintenance of homeostasis in the GI tract. Activation of the intestinal opioid receptors (ORs), in particular μ (MOP) and δ (DOP) results in reduction of epithelial secretion and increase of water/electrolyte absorption; moreover, opioids are strong analgesic agents. Thus, ligands of ORs are a promising target in IBS-D treatment. In this review, we discuss the role of ORs in the pathogenesis of IBS-D and the use of “classical” and novel, such as P-317, eluxadoline and biphalin MOP and DOP receptor ligands in preclinical and clinical trials.
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Cite this article as:
Jarmuż Agata, Zielińska Marta, Leń Karolina, Banaszek Martyna, Storr Martin and Fichna Jakub, Review: The Role of MOP and DOP Receptors in Treatment of Diarrheapredominant Irritable Bowel Syndrome, Mini-Reviews in Medicinal Chemistry 2016; 16 (18) . https://dx.doi.org/10.2174/1389557516666160804165318
DOI https://dx.doi.org/10.2174/1389557516666160804165318 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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