货号:A455841 同义名: 福沙吡坦二甲葡胺 / MK-0517;L785298
Fosaprepitant Dimeglumine is a prodrug for aprepitant which is a selective and high-affinity antagonist of NK1 receptor.
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描述 | Known to induce vomiting, substance P binds to NK-1 receptors in the abdominal vagus, the NTS and the area postrema. Compounds that block NK-1 receptors lessen emesis after cisplatin, ipecac, apomorphine and radiation therapy[3]. Aprepitant is a selective NK-1 receptor antagonist approved as a therapy for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). Fosaprepitant is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min via the action of ubiquitous phosphatases[3]. Injection of the NK-1 receptor antagonists fosaprepitant directly into the vicinity of the NTS neurons inhibited cisplatin-induced emesis in the ferret, which suggested fosaprepitant may exert its main anti-emetic action centrally by depressing the neural activity of the NTS neurons, with possibly some peripheral anti-emetic effect through blockade of NK-1 receptors located on vagal terminals in the gut[3]. Preclinical toxicology studies of bolus fosaprepitant administered in seconds to dogs and rats showed that concentrations of 1 mg/ml were well tolerated. Concentrations up to 25 mg/ml at low doses (2 – 4 mg/kg/day) were well tolerated in dog[4]. |
Dose | Rat: 1 mg/kg, 8 mg/kg[3] (i.v.) |
Administration | i.v. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00090207 | Nausea Vomiti... 展开 >>ng 收起 << | Phase 4 | Completed | - | - |
NCT00726960 | Opioid-Related Disorders ... 展开 >> Heroin Dependence Substance-Related Disorders 收起 << | Phase 1 | Unknown | June 2010 | Sweden ... 展开 >> Karolinska University Hospital, Huddinge Stockholm, Sweden, 14186 收起 << |
NCT00717054 | Nausea Vomiti... 展开 >>ng 收起 << | Not Applicable | Completed | - | United States, Pennsylvania ... 展开 >> Hahnemann University Hospital Philadelphia, Pennsylvania, United States, 19102 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.00mL 0.20mL 0.10mL |
4.98mL 1.00mL 0.50mL |
9.95mL 1.99mL 1.00mL |
CAS号 | 265121-04-8 |
分子式 | C37H56F7N6O16P |
分子量 | 1004.834 |
别名 | 福沙吡坦二甲葡胺 ;MK-0517;L785298;Fosaprepitant dimeglumine salt |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
H2O: 50 mg/mL(49.76 mM),配合低频超声助溶 |
动物实验配方 |