chemical
Pharmacological action and mechanism Meclizine hydrochloride is an antagonist of histamine receptor, which can antagonize the hypotensive effect caused by histamine, protect animals from death caused by Lethal dose histamine, and has central inhibition and local anesthesia effects. Indicative treatment and prevention of motion sickness causing nausea, vomiting, and dizziness. Precautions 1) Be cautious when using bladder neck stenosis, benign prostatic hypertrophy, angle closure glaucoma, pyloric duodenal stenosis, etc. 2) Meclizine Hydrochloride Chemalbook can inhibit the skin reaction caused by histamine. It should be stopped 72 hours before the Drug allergy skin test to avoid false negative reaction results. Biological activity Melizine (NSC28728) is a histamineH1receptor antagonist, which is used to treat nausea and Motion sickness. It is also an agonist ligand of mCAR (constitutive androgen receptor agonist ligand) and a Inverse agonist of hCAR.
In vitro study, Meclizine is a histamine H1 receptor antagonist, used to treat nausea and Motion sickness, with anticholinergic, central nervous system inhibition and local anesthesia effects. Meclizine is a mouse CAR agonist ligand (constitutive androstane receptor) and a human CAR Inverse agonist. In vitro experiments, Meclizine dose dependently increased the trans activation of mCAR and activated the binding of Hormone receptor coactivator 1 to the receptor. On the contrary, in liver cells derived from mice that only express hCAR and Chemicalbook does not express mCAR, meclizine inhibits hCAR transcriptional activation and the expression of Rumina induced CAR downstream genes, including cytochrome p450 monooxygenase (CYP) 2B10, CYP3111, and CYP1A2. In vivo studies have shown that treating mice with Meclizine increases the expression of CAR target genes in a CAR dependent manner. In the mouse polyQ toxic cell model, Meclizine reduces oxidative metabolism and inhibits apoptotic cell death.