Home Neuronal Signaling Histamine Receptor antagonist - CAR agonist Meclizine 2HCl For research use only.

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 No. 1104-22-9

Purity & Quality Control

Meclizine 2HCl Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

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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