Meclizine dihydrochloride

SKU: orb1226981

Description

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.

Key Properties

• CAS Number: 1104-22-9
• MW: 463.87
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₇ClN₂·2HCl
• SMILES: Cl.Cl.CC1=CC(CN2CCN(CC2)C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)=CC=C1
• Target: Histamine Receptor
• Solubility: DMSO: 1 mg/mL (2.15 mM)

Bioactivity

• 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. 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.
• 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. Cell Viability Assay Cell line: The murine striatal cells expressing wild-type (STHdhQ7/7) or mutant (STHdhQ111/111) huntingtin protein. Concentration: 50 μM. Incubation 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 28728

Quick Database Links

Gene Symbol

Histamine Receptor