Abstract
Background: 5-HT4 receptor plays important roles regulating gastrointestinal motility, enteric neuronal signaling and visceral pain in the gastrointestinal tract. Over the past decade, the 5-HT4 receptor has been highlighted as an attractive drug target for the treatment of gastrointestinal motility disorders such as irritable bowel syndrome, chronic constipation, functional dyspepsia, gastroparesis and so on. Objectives: This article aims to provide an overview of serotonin receptors related to the gastrointestinal motility disorders, and to address the characteristics of past, current and future 5-HT4 receptor agonists for treatment of functional gastrointestinal disorders, focusing on the pharmacology, efficacy and safety profile.
Highlights
Gastrointestinal (GI) motility disorder including irritable bowel syndrome, chronic constipation, functional dyspepsia and gastroparesis is a common and debilitating disease that has a profound effect on patient’s quality of life and imposes a substantial economic burden
According to predominant bowel habit disturbance, Irritable bowel syndrome (IBS) patients were classified as IBS with constipation (IBS-C), IBS with diarrhea (IBS-D) and mixed form (IBS-M)
In phase III clinical trials for 12 weeks in patients with chronic idiopathic constipation (> 1977 patients) [85,86,87], the patients treated with prucalopride reported a statistically significant (p
Summary
Gastrointestinal (GI) motility disorder including irritable bowel syndrome, chronic constipation, functional dyspepsia and gastroparesis is a common and debilitating disease that has a profound effect on patient’s quality of life and imposes a substantial economic burden. Irritable bowel syndrome (IBS) is characterized by abnormalities in motility and visceral hypersensitivity [1]. The underlying cause is thought to involve dysfunction in GI motility, psychological factors, hypersensitivity and inflammation of the bowel, and aberrant autonomic function. Patients with IBS reported considerable impairments in health status having poor health-related quality of life (HRQOL) with dietary restrictions, mood disturbance and interference with daily activity and severe symptoms as pain, bowel difficulties, bloating and eating/dietary restrictions [6,7]
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