Meclizine dihydrochloride 是一种组胺 H1 拮抗剂,用于治疗妊娠期间的晕动病、眩晕和恶心以及放射病。它是小鼠组成型雄甾烷受体激动剂,是人 CAR 的反向激动剂。它可透过血脑屏障,可用于多聚谷氨酰胺毒性障碍方面的研究。
产品描述
Meclizine hydrochloride is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.
体外活性
Meclizine以CAR依赖的方式增加小鼠CAR靶基因的表达.
体内活性
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。
细胞实验
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)
Cas No.
1104-22-9
分子式
C25H27ClN2
分子量
463.87
别名
NSC28728;盐酸美克洛嗪;Meclozine dihydrochloride;Meclizine 2HCl
储存和溶解度
DMSO:23.2 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years