Velusetrag
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| Velusetrag | |
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N-((1R,3R,5S)-8-((R)-2-Hydroxy-3-(N-methylmethylsulfonamido)propyl)-8-azabicyclo[3.2.1]octan-3-yl)-1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
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Other names
TD-5108
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| Identifiers | |
| CAS number | 866933-46-2  , 866933-51-9 (HCl) |
| UNII | J4VNV64ARB |
| Jmol-3D images | Image 1 |
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| Properties | |
| Molecular formula | C25H36N4O5S |
| Molar mass | 504.64 g mol−1 |
 (verify) (what is:  / ?)Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) |
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| Infobox references |
Velusetrag is an experimental drug candidate for the treatment of chronic constipation and irritable bowel syndrome.[1] It is a selective 5-HT4 receptor agonist.[2]
In clinical trials, velusetrag was efficacious and well tolerated in patients with chronic constipation,[3] and showed accelerated intestinal and colonic transit after single dosing and accelerated gastric emptying after multiple dosing.[4]
[edit] See also
[edit] References
- ^ M. Vazquez-Roque, and M. Camilleri (2011). "Velusetrag". Drugs of the Future 36 (6): 447–454. doi:10.1358/dof.2011.36.6.1594078.
- ^ Smith, JA; Beattie, DT; Marquess, D; Shaw, JP; Vickery, RG; Humphrey, PP (2008). "The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity". Naunyn-Schmiedeberg's archives of pharmacology 378 (1): 125–37. doi:10.1007/s00210-008-0282-y. PMID 18415081.
- ^ Goldberg, M; Li, YP; Johanson, JF; Mangel, AW; Kitt, M; Beattie, DT; Kersey, K; Daniels, O (2010). "Clinical trial: The efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation - a 4-week, randomized, double-blind, placebo-controlled, dose-response study". Alimentary pharmacology & therapeutics 32 (9): 1102–12. doi:10.1111/j.1365-2036.2010.04456.x. PMID 21039672.
- ^ Manini, ML; Camilleri, M; Goldberg, M; Sweetser, S; McKinzie, S; Burton, D; Wong, S; Kitt, MM et al. (2010). "Effects of Velusetrag (TD-5108) on gastrointestinal transit and bowel function in health and pharmacokinetics in health and constipation". Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society 22 (1): 42–9, e7–8. doi:10.1111/j.1365-2982.2009.01378.x. PMC 2905526. PMID 19691492. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2905526.
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