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.
| Cell Experiment | |
|---|---|
| Cell lines | HepG2 cells |
| Preparation method | 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. |
| Concentrations | ~10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Mouse |
| Formulation | corn oil |
| Dosages | 100 mg/kg |
| Administration | i.p. |
| Molecular Weight | 463.87 |
| Formula | C25H27Cl2N2.2HCl |
| CAS Number | 1104-22-9 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Bobby T. Houston, et al. Meclizine
[2] No authors listed. Antiemetic Agents
[3] No authors listed. Meclizine
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