Meclizine 2HCl

Catalog No.S1986 Synonyms: NSC 28728

Meclizine 2HCl Chemical Structure

Molecular Weight(MW): 463.87

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.

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Biological Activity

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.
Targets
Histamine H1 receptor [1]
In vitro

Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects. [1] 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. [2]

In vivo Meclizine administration to mice increases expression of CAR target genes in a CAR-dependent manner. [2] Meclizine silence oxidative metabolism, suppresses apoptotic cell death in a murine cellular model of polyglutamine (polyQ) toxicity. [3]

Protocol

Cell Research:[2]
+ Expand
  • Cell lines: HepG2 cells
  • Concentrations: ~10 μM
  • Incubation Time: 24 h
  • Method: HepG2 cells are cultured in 24-well dishes with DMEM supplemented with 10% charcoal-stripped calf serum. Cells are transfected using calcium phosphate with 100 ng of receptor expression vectors, 300 ng of luciferase reporter plasmids, and 100 ng of pSV2-β-galactosidase as internal control of transfection efficiency. Drugs are added 12 h after transfection, and cells are incubated for an additional 24 h. The cell lysate is assayed for luciferase activity and normalized to β-galactosidase activity.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Mouse
  • Formulation: corn oil
  • Dosages: 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (8.62 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+95% Corn oil
10 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 463.87
Formula

C25H27Cl2N2.2HCl

CAS No. 1104-22-9
Storage powder
Synonyms NSC 28728

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02112578 Recruiting Vertigo, Peripheral Apsen Farmaceutica S.A. November 2016 Phase 3
NCT02625181 Recruiting Postoperative Nausea and Vomiting Vanderbilt University|University of Washington July 2016 --
NCT01537471 Completed Healthy Duke University|Wallace H. Coulter Foundation January 2012 Phase 1
NCT01443858 Completed Smoking Cessation Duke University|Philip Morris USA, Inc. August 2011 Phase 2
NCT00641797 Completed Benign Paroxysmal Positional Vertigo Lehigh Valley Hospital November 2006 --

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID