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Meclizine dihydrochloride
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产品介绍
产品介绍
产品信息
抗原名称
Histamine H1 receptor
商品描述
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.
分子量
463.87
纯度
>98%
可溶性
DMSO ：23.2 mg/mL (50 mM)
外观
白色结晶性粉末
In vitro(体外研究)
Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine is an agonist ligand for mouse CAR (constitutive androstane receptor), and an inverse agonist for human CAR. Meclizine increases mCAR transactivation in a dose-dependent manner, stimulates binding of steroid receptor coactivator 1 to the murine receptor in vitro. In contrast, meclizine suppresses hCAR transactivation and inhibits the phenobarbital-induced expression of the CAR target genes, cytochrome p450 monooxygenase (CYP)2B10, CYP3A11, and CYP1A2, in primary hepatocytes derived from mice expressing hCAR, but not mCAR.
In vivo(体内研究)
Meclizine administration to mice increases expression of CAR target genes in a CAR-dependent manner. Meclizine silence oxidative metabolism, suppresses apoptotic cell death in a murine cellular model of polyglutamine (polyQ) toxicity.
背景
别名
盐酸美克洛嗪；Meclozine dihydrochloride； NSC28728
分子式
C25H27Cl2N2.2HCl
CAS号
1104-22-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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