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夫罗曲坦琥珀酸盐  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： F10332 产品名称： Frovatriptan succinate CAS: 158930-09-7   储存条件 粉末 -20℃ 四年     分子式： C18H23N3O5 溶于液体 -80℃ 两年 分子量 361.39     化学名：  butanedioic acid;(6R)-6-(methylamino)-6,7,8,9-tetrahydro-5H-carbazole-3-carboxamide Solubility (25°C)：   体外:   DMSO 72 mg/mL (199.23mM) Water 72 mg/mL (199.23mM) Ethanol Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7671mL 13.8355mL 27.6709mL 5mM 0.5534mL 2.7671mL 5.5342mL 10mM 0.2767mL 1.3835mL 2.7671mL 50mM 0.0553mL 0.2767mL 0.5534mL   生物活性 产品描述 一种强效，高亲和力，选择性和具有口服活性的 5-HT1B (pK50 为 8.2) 和 5-HT1D 受体激动剂，选择性是 5-HT1A，5-HT1F 和 5-HT7 的 10 倍以上，是其他 5-HT，多巴胺，组胺 H1 和 α1-肾上腺素受体的 1000 倍以上。Frovatriptan succinate 可用于偏头痛的研究。 靶点 5-HT1B Receptor 8.2 (pEC50) 5-HT1D Receptor   体外研究 Cerebral vasodilatation and neurogenic inflammation are considered to be prime movers in the pathogenesis of migraine. Activation of 5-HT1B reverses cerebral vasodilatation and activation of 5-HT1D prevents neurogenic inflammation. Frovatriptan has a high affinity for 5-HT1B and 5-HT1D receptors and a moderate affinity for the 5-HT1A and 5-HT1F receptors subtypes. Frovatriptan has a moderate affinity for the 5-HT7 receptors, an action associated with coronary artery relaxation in the dog. 体内研究 Oral bioavailability of Frovatriptan is 22%-30% and is not affected by food. Although the maximum concentration in the plasma is achieved in 2-3 hours, 60%-70% of this is achieved in 1 hour. A steady state is achieved in 4-5 days. Plasma protein binding is low at 15%. The most unique feature is the relative terminal long half-life of about 26 hours. Frovatriptan is chiefly metabolized by CYP1A2 and is cleared by the kidney and liver making moderate failure of either organ not a limiting factor in treatment. Frovatriptan (0.1, 0.2, and 0.3 mg/kg; a single bolus intraduodenal administration) treatment produces an increase in carotid vascular resistance, which is sustained for at least 5 hours in dogs.
保存条件：-20℃

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