Synonyms: compound 15 [PMID 22959244] | TD-5108
Compound class:
Synthetic organic
Comment: Velusetrag is a potent and selective, orally available agonist of the 5-HT4 receptor. The compound is being investigated as a treatment for chronic constipation [6,8] and irritable bowel syndrome [7].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use ![]() |
Velusetrag has reached Phase 2 clinical trial. |
Mechanism Of Action and Pharmacodynamic Effects ![]() |
The 5-HT4 receptor subtype is physiologically and pathophysiologically important for the regulation of intestinal peristalsis and gut motility [1,4-5]. Activation of these receptors in the gut wall enhances the peristaltic reflex [2], relaxes the smooth muscle and increases fluid secretion in the gastrointestinal (GI) tract [3]. All of these actions improve transit in GI functional disorders. |