Pumosetrag Hydrochloride (MKC-733) |
| カタログ番号GC31393 |
Pumosetrag Hydrochloride (MKC-733) (MKC-733; DDP-733) は、過敏性腸症候群および胃食道逆流症の治療のために開発された経口投与可能な 5-HT3 部分アゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 194093-42-0
Sample solution is provided at 25 µL, 10mM.
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Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
Pumosetrag displays both regional and species specificities. Pumosetrag has a lower efficacy than 5-HT in the rat jejunum, ileum and distal colon; however, it has similar efficacy and potency to 5-HT in the rat proximal colon. The activity profile of Pumosetrag is different in the guinea pig intestine where it exhibits greater potency and efficacy than 5-HT in all regions. Pumosetrag shows little to no response in the regions of the mouse intestine. Responses to Pumosetrag in the rat and guinea pig tissues are inhibited by ondansetron, confirming its action on 5-HT(3) receptors[1]. Pumosetrag delays liquid gastric emptying in association with relaxation of the proximal stomach, stimulates fasting antroduodenal migrating motor complex activity and accelerates small intestinal transit[2].
[1]. Chetty N, et al. Effects of the novel 5-HT3 agonist MKC-733 on the rat, mouse and guinea pig digestive tract. Pharmacology. 2008;81(2):104-9. Epub 2007 Oct 19. [2]. Coleman NS, et al. Effect of a novel 5-HT3 receptor agonist MKC-733 on upper gastrointestinal motility in humans. Aliment Pharmacol Ther. 2003 Nov 15;18(10):1039-48.
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