| 货号 | 14692-5mg |
| 描述 | Tegaserod (maleate) is a potent agonist of the serotonin 4 receptor (5-HT4, Ki = 3.9-31 nM).1,2 As 5-HT4 receptors are associated with cholinergic nerves lining the colon, tegaserod (maleate) stimulates colonic motility and transit in vivo, in both healthy and diseased gastrointestinal tracts.3,4 However, it lacks selectivity, since it also acts as an antagonist for the 5-HT2A, 5-HT2B, and 5-HT2C receptors (Ki = 32, 3.9, and 100 nM, respectively).5,6,4 It is a weak agonist of 5-HT3(Ki ≤ 10 μM).7 |
| 别名 | SDZ-HTF 919;Zelnorm; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Long, D.D.,Armstrong, S.R.,Beattie, D.T., et al. Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. Bioorganic & Medicinal Chemistry Letters 22(19), 6048-6052 (2012). 2.Hedner, E.,Sjögren, M.,Frändberg, P.A., et al. Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. Journal of Natural Products 69(10), 1421-1424 (2006). 3.Nguyen, A.,Camilleri, M.,Kost, L.J., et al. SDZ HTF 919 stimulates canine colonic motility and transit in vivo. Journal of Pharmacology and Experimental Therapeutics 280(3), 1270-1276 (1997). 4.Tack, J.,Camilleri, M.,Chang, L., et al. Systematic review: Cardiovascular safety profile of 5-HT4 agonists developed for gastrointestinal disorders. Alimentary Pharmacology and Therapeutics 35(7), 745-767 (2012). 5.Beattie, D.T.,Smith, J.A.M.,Marquess, D., et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. British Journal of Pharmacology 143(5), 549-560 (2004). 6.McCullough, J.L.,Armstrong, S.R.,Hegde, S.S., et al. The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat. Pharmacological Research 53(4), 353-358 (2006). 7.Lemaître, S.,Lepailleur, A.,Bureau, R., et al. Novel antagonists of serotonin-4 receptors: Synthesis and biological evaluation of pyrrolothienopyrazines. Bioorganic & Medicinal Chemistry 17(6), 2607-2622 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 417.5 |
| 分子式 | C16H23N5O • C4H4O4 |
| CAS号 | 189188-57-6 |
| 稳定性 | ≥ 2 years |
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