| 产品描述: | 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. |
| 靶点: |
5-HT3 Receptor;5-HTReceptor |
| 体内研究: |
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. 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 |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.943 ml |
14.713 ml |
29.426 ml |
| 5 mM |
0.589 ml |
2.943 ml |
5.885 ml |
| 10 mM |
0.294 ml |
1.471 ml |
2.943 ml |
| 50 mM |
0.059 ml |
0.294 ml |
0.589 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |