生物活性
Ondansetron (Zofran) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic. Its effects are thought to be on both peripheral and central nerves. Ondansetron (Zofran) decreases the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also inhibits serotonin receptors in the chemoreceptor trigger zone. Ondansetron (Zofran) has little effect on vomiting caused by motion sickness, and does not have any effect on dopamine receptors or muscarinic receptors. The 5-HT3 receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting (CINV). Ondansetron (Zofran) is also effective in controlling post-operative nausea and vomiting (PONV) and post-radiation nausea and vomiting, and is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis. Although ondansetron is highly effective, the high cost of the brand-name version had limited its use to controlling PONV and CINV.Ondansetron (Zofran) is also used off-label to treat hyperemesis gravidarum in pregnant women, but there is no conclusive data available on its safety in pregnancy, especially during the first trimester. Ondansetron (Zofran) is also used to treat cyclic vomiting syndrome.
化学数据
分子量 | 293.36 |
分子式 | C18H19N3O |
CAS号 | 99614-02-5 |
纯度 | >98% |
溶解性(25°C) | DMSO |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.4088 mL | 17.0439 mL | 34.0878 mL |
5 mM | 0.6818 mL | 3.4088 mL | 6.8176 mL |
10 mM | 0.3409 mL | 1.7044 mL | 3.4088 mL |