生物活性
Meclizine dihydrochloride is a human pregnane X receptor (hPXR) agonist and histamine H1 receptor antagonist. Meclizine dihydrochloride is stronger activator of hPXR than rat PXR. Meclizine dihydrochloride increases hPXR target gene expression in human hepatocyte primary cultures. Meclizine dihydrochloride is an antihistamine considered to be an antiemetic. Meclizine dihydrochloride possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine dihydrochloride depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. Meclizine dihydrochloride is used to treat or prevent nausea, vomiting, and dizziness caused by motion sickness.
化学数据
| 分子量 | 463.87 |
| 分子式 | C25H27Cl2N2.2HCl |
| CAS号 | 1104-22-9 |
| 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 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | HepG2 cells |
| 方法 | Culturing HepG2 cells in 24-well dishes with DMEM supplemented with 10% charcoal-stripped calf serum. Using calcium phosphate with 100 ng of receptor expression vectors to transfect cells , 300 ng of luciferase reporter plasmids, and 100 ng of pSV2-β-galactosidase as internal control of transfection efficiency. 12 h after transfection,adding the drugs, and incubating cells for an additional 24 h. The cell lysate is assayed for luciferase activity and normalized to β-galactosidase activity. |
| 浓度 | ~10 μM |
| 处理时间 | 24 h |
| 动物实验 |
|---|
| 动物模型 | Mouse |
| 配制 | corn oil |
| 剂量 | 100 mg/kg |
| 给药处理 | i.p. |
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 | 2.1558 mL | 10.7789 mL | 21.5578 mL |
| 5 mM | 0.4312 mL | 2.1558 mL | 4.3116 mL |
| 10 mM | 0.2156 mL | 1.0779 mL | 2.1558 mL |
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