Meclizine 2HCl

Synonyms: NSC 28728,Meclozine dihydrochloride

Meclizine (NSC 28728,Meclozine dihydrochloride) 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.

Meclizine 2HCl Chemical Structure

Meclizine 2HCl Chemical Structure

CAS: 1104-22-9

Selleck's Meclizine 2HCl has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

Meclizine 2HCl Related Products

Choose Selective Histamine Receptor Inhibitors

Biological Activity

Description Meclizine (NSC 28728,Meclozine dihydrochloride) 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
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]

Cell Research 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.

In Vivo
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]

Animal Research Animal Models Mouse
Dosages 100 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04482985 Unknown status
Seasickness|Meclizine
Medical Corps Israel Defense Force
September 1 2020 Phase 4
NCT04564144 Unknown status
Emesis
Mansoura University
June 1 2020 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 463.87 Formula

C25H27Cl2N2.2HCl

CAS No. 1104-22-9 SDF Download Meclizine 2HCl SDF
Smiles CC1=CC(=CC=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 2 mg/mL

DMSO : 1 mg/mL ( (2.15 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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