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Fosaprepitant Dimeglumine

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Chemical Structure| 265121-04-8 同义名 : 福沙吡坦二甲葡胺 ;MK-0517;L785298;Fosaprepitant dimeglumine salt
CAS号 : 265121-04-8
货号 : A455841
分子式 : C37H56F7N6O16P
纯度 : 98%
分子量 : 1004.834
MDL号 : MFCD23102059
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(49.76 mM)，配合低频超声助溶
动物实验配方：
生物活性
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].
临床研究
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 <<
实验方案
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
参考文献

[1]Grunberg S, Chua D, et al. Single-dose fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with cisplatin therapy: randomized, double-blind study protocol--EASE. J Clin Oncol. 2011 Apr 10;29(11):1495-501.

[2]Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6.

[3]Navari RM. Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Expert Opin Investig Drugs. 2007 Dec;16(12):1977-85. doi: 10.1517/13543784.16.12.1977. PMID: 18042005.

[4]Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6. doi: 10.2147/tcrm.s2345. PMID: 18728837; PMCID: PMC2504061.