Meclizine dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Meclizine 是一种组胺 H1 受体拮抗剂，用于治疗恶心和晕动病，具有抗组胺、抗毒蕈碱和抗氧化磷酸化特性。

Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR.(In Vitro):Meclizine (Meclozine; 50 μM; 24 hours) dihydrochloride significantly increases cell survival in STHdhQ111/111 cells at 24 h after the removal of serum, evidently by suppressing apoptosis, based on caspase 3 and 7 cleavage. The rescue is dose-dependent with an EC50 of 17.3 μm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine dihydrochloride protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells.(In Vivo):Meclizine (Meclozine; 10-100 mg/kg; ip) dihydrochloride protects mouse against kidney ischemia. Pretreatment with 100 mg/kg of Meclizine, 17 or 24 h prior to ischemia shows kidney protection in mice. Meclizine dihydrochloride reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis.

Meclizine (Meclozine; 50 μM; 24 hours) dihydrochloride significantly increases cell survival in STHdhQ111/111 cells at 24 h after the removal of serum, evidently by suppressing apoptosis, based on caspase 3 and 7 cleavage. The rescue is dose-dependent with an EC50 of 17.3 μm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine dihydrochloride protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells. Cell Viability Assay Cell Line:The murine striatal cells expressing wild-type (STHdhQ7/7) or mutant (STHdhQ111/111) huntingtin protein Concentration:50 μMIncubation Time:24 hours Result:Significantly increased cell survival in STHdhQ111/111 cells at 24 h after the removal of serum. Western Blot Analysis Cell Line:Mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells.

Meclizine (Meclozine; 10-100 mg/kg; ip) dihydrochloride protects mouse against kidney ischemia. Pretreatment with 100 mg/kg of Meclizine, 17 or 24 h prior to ischemia shows kidney protection in mice. Meclizine dihydrochloride reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis. Animal Model:8-10 wk old male C57BL/6 mice Dosage:10, 30, 60 or 100 mg/kg Administration:Administered intraperitoneally Result:Protected mice from kidney ischemia-reperfusion injury.

NSC 28728

GPCR/G Protein

Histamine Receptor

H1 receptor

Neurological Disease

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1104-22-9

463.87

C25H27ClN2·2HCl

>98% (HPLC)

DMSO: 1 mg/mL (2.15 mM)

Cl.Cl.CC1=CC(CN2CCN(CC2)C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years