Synonyms: compound 18 [PMID 23756062]
Compound class:
Synthetic organic
Comment: TD-8954 is a potent and selective agonist of the 5-HT4 receptor [2,7]. The compound is being investigated for its gastrointestinal prokinetic action.
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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References |
1. Baker DE. (2005)
Rationale for using serotonergic agents to treat irritable bowel syndrome. Am J Health Syst Pharm, 62 (7): 700-11; quiz 712-3. [PMID:15790796] |
2. Beattie DT, Armstrong SR, Vickery RG, Tsuruda PR, Campbell CB, Richardson C, McCullough JL, Daniels O, Kersey K, Li YP et al.. (2011)
The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol, 2: 25. [PMID:21687517] |
3. Gershon MD, Tack J. (2007)
The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gastroenterology, 132 (1): 397-414. [PMID:17241888] |
4. Hansen MB, Skadhauge E. (1997)
Signal transduction pathways for serotonin as an intestinal secretagogue. Comp Biochem Physiol A Physiol, 118 (2): 283-90. [PMID:9366057] |
5. Kadowaki M, Wade PR, Gershon MD. (1996)
Participation of 5-HT3, 5-HT4, and nicotinic receptors in the peristaltic reflex of guinea pig distal colon. Am J Physiol, 271 (5 Pt 1): G849-57. [PMID:8944700] |
6. Kim DY, Camilleri M. (2000)
Serotonin: a mediator of the brain-gut connection. Am J Gastroenterol, 95 (10): 2698-709. [PMID:11051338] |
7. McKinnell RM, Armstrong SR, Beattie DT, Fatheree PR, Long DD, Marquess DG, Shaw JP, Vickery RG. (2013)
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties. Bioorg Med Chem Lett, 23 (14): 4210-5. [PMID:23756062] |