Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Meclizine以CAR依赖的方式增加小鼠CAR靶基因的表达.

Meclizine在体外实验中,剂量依赖性增加mCAR反式激活,激活激素受体共激活因子1与受体的结合。相反,Meclizine在来源于小鼠的只表达hCAR,不表达mCAR的肝脏细胞中,抑制hCAR转录激活和鲁米那诱导的CAR下游基因（包括细胞色素p450 单氧酶2B10、CYP3A11以及CYP1A2）的表达。Meclizine是小鼠CAR激动剂配体(组成型雄甾烷受体),人类CAR的反向激动剂。

HepG2 cells are cultured in 24-well dishes with DMEM supplemented with 10% charcoal-stripped calf serum. Cells are transfected using calcium phosphate with 100 ng of receptor expression vectors, 300 ng of luciferase reporter plasmids, and 100 ng of pSV2-β-galactosidase as internal control of transfection efficiency. Drugs are added 12 h after transfection, and cells are incubated for an additional 24 h. The cell lysate is assayed for luciferase activity and normalized to β-galactosidase activity.(Only for Reference)