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| 品牌 | absin | CAS | 189188-57-6 |
|---|---|---|---|
| 分子式 | C20H27N5O5 | 纯度 | ＞98% |
| 分子量 | 417.46 | 货号 | abs47027753 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | used for the management of irritable bow | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Tegaserod maleate 189188-57-6
| 产品描述 | |
| 描述 | Tegaserod is a 5-HT4 agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation. Its use was the only drug approved by the United States Food and Drug Administration to help relieve the abdominal discomfort, bloating and constipation associated with irritable bowel syndrome. On March 30, 2007, the U.S. Food and Drug Administration requested that Novartis withdraw Zelnorm from shelves. The FDA alleges a relationship between prescriptions of the drug and increased risks of heart attack or stroke. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 马来酸替加色罗；SDZ-HTF-919；HTF-919 |
| 外观 | 类白色结晶粉末 |
| 可溶性/溶解性 | DMSO : ≥ 35 mg/mL (83.84 mM) |
| 生物活性 | |
| 靶点 | 5-HT4 receptor |
| In vitro(体外研究) | In guinea-pig and rat colon, luminal application of tegaserod activates 5-HT4 receptors on intrinsic primary sensory neurons that release calcitonin gene-related peptide which in turn activates cholinergic interneurons stimulating the peristaltic reflex. In isolated segments of guinea-pig colon, intralumnal tegaserod increased the velocity of propulsion of artificial faecal pellets through the stimulation of the same receptor. In rat distal colon, intraluminal tegaserod stimulated 5-HT4 4 receptors on colonocytes to secrete chloride and water through an adenylyl cyclase-dependent pathway. |
| In vivo(体内研究) | In a study in dogs tegaserod 0.1 or 0.3 mg/kg i.v. increased the motility of the antrum, duodenum and jejunum in both fasting and fed conditions. In a model of delayed gastric emptying, the same doses of tegaserod restored normal gastric transit time. Tegaserod 0.3 mg/kg in rats was able to increase gastric and small bowel motility while in a model of postoperative ileus it was able to restore gastric motility. In humans, pharmacokinetic analysis reveals that tegaserod is rapidly absorbed following oral administration. Absolute bioavailability is 11 ± 3% and is decreased by 50% under fed conditions. The time to reach peak plasma concentration ranges from 1-1.3 h. In the bloodstream, tegaserod is predominantly bound by α1-glycoprotein and does not cross the blood-brain barrier to any significant extent. The terminal elimination half time is 11 ± 5 h. Age and gender do not influence the pharmacokinetics of tegaserod and tegaserod has the potential for good tolerability. |
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| 研究领域 | |
| 研究领域 | MetabolismTypes of diseaseObesity NeuroscienceProcesses NeuroscienceNeurology processMetabolism NeuroscienceNeurotransmissionReceptors / ChannelsGPCRSerotonin Receptors Signal TransductionSignaling PathwayG Protein SignalingGPCR Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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