1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis
  2. Histamine Receptor Apoptosis
  3. Meclizine

Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease.

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Meclizine Chemical Structure

Meclizine Chemical Structure

CAS No. : 569-65-3

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Description

Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease[1][2][3].

IC50 & Target[1]

H1 Receptor

 

In Vitro

Meclizine (Meclozine; 50 μM; 24 hours) significantly increases cell survival in STHdh 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 protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

Cell Line: Mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells
Concentration: 50 µM
Incubation Time: 0, 4, 10, 24 hours
Result: Suppressed apoptosis, based on caspase 3 and 7 cleavage.
In Vivo

Meclizine (Meclozine; 10-100 mg/kg; ip) 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 reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-10 wk old male C57BL/6 mice[4]
Dosage: 10, 30, 60 or 100 mg/kg
Administration: Administered intraperitoneally
Result: Protected mice from kidney ischemia-reperfusion injury.
Molecular Weight

390.95

Formula

C25H27ClN2

CAS No.
SMILES

CC1=CC(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)=CC=C1

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Meclizine
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HY-B0349A
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