| 货号 | 21657-5mg |
| 描述 | Cisapride is a selective agonist of the serotonin receptor (5-HT) subtype 5-HT4, but it also exhibits weak inhibitory activity towards 5-HT3.1,2 Cisapride has an IC50 value of 0.483 μM at 5-HT4, as measured in a Cos-7 receptor binding assay, while in an esophageal contraction assay it has a pEC50 value of 6.99.3In vivo, cisapride is a gastroprokinetic agent, increasing contractility and motility within the gastrointestinal tract.2 Cisapride also induces heart arrhythmia, which is linked to its inhibition of the cardiac K+ channel subunit Kv11.1, encoded by the human Ether-à-go-go-Related Gene (HERG), with an IC50 value of <1 μM.4,3 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Taniyama, K.,Nakayama, S.,Takeda, K., et al. Cisapride stimulates motility of the intestine via the 5-hydroxytryptamine receptors. J. Pharm. Exp. Ther. 258(3), 1098-1104 (1991). 2.Linnik, M.D.,Butler, B.T.,Gaddis, R.R., et al. Analysis of serotonergic mechanisms underlying benzamide-induced gastroprokinesis. J. Pharmacol. Exp. Ther. 259(2), 501-507 (1991). 3.Park, J.S.,Im, W.,Choi, S., et al. Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. Eur. J. Med. Chem. 109, 75-88 (2016). 4.Rampe, D.,Roy, M.-L.,Dennis, A., et al. A mechanism for the proarrhythmic effects of cisapride (Propulsid): High affinity blockade of the human cardiac potassium channel HERG. FEBES Lett. 417(1), 28-32 (1997). | |
| 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 | 466 |
| 分子式 | C23H29ClFN3O4 |
| CAS号 | 81098-60-4 |
| 稳定性 | ≥ 2 years |
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