Meclizine dihydrochloride

SKU: orb1309739

Description

Meclizine dihydrochloride (NSC28728) is a histamine H1 receptor antagonist. It is utilized in research on motion sickness, vertigo, and nausea, with applications in neuropharmacology and vestibular studies. Its mechanisms are investigated in both in vivo models and in vitro receptor binding assays.

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1104-22-9
• MW: 463.87
• Purity: 95.41% (May vary between batches)
• Formula: C₂₅H₂₇ClN₂·2HCl
• SMILES: c1(cc(ccc1)C)CN1CCN(C(c2ccc(cc2)Cl)c2ccccc2)CC1.Cl.Cl
• Target: Apoptosis,Histamine Receptor
• Solubility: DMSO:15 mg/mL (32.34 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.31 mM)

Bioactivity

• In Vivo:
  In vitro, Meclizine exhibits dose-dependent augmentation of mCAR transactivation and enhances the recruitment of the coactivator SRC-1 (steroid receptor coactivator-1) to the receptor. Conversely, in mouse hepatocytes expressing only hCAR and not mCAR, Meclizine inhibits hCAR transcriptional activation and suppresses the expression of luminal-induced CAR downstream genes, which include CYP2B10, CYP3A11, and CYP1A2 (cytochrome P450 monooxygenases). Therefore, Meclizine acts as an agonist ligand for mouse CAR (constitutive androstane receptor) but as a reverse agonist for human CAR.
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• In Vitro:
  Meclizine increases the expression of mouse CAR target genes in a CAR-dependent manner.
• Cell Research:
  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)
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Storage & Handling

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

Alternative Names

inhibit, NSC 28728, NSC28728, NSC-28728, H1 receptor, HistamineReceptor, Histamine Receptor, Meclizine, Meclizine 2HCl, Meclizine dihydrochloride, Meclizine Dihydrochloride, Meclozine, Meclozine dihydrochloride, Meclozine Dihydrochloride, Inhibitor, Huntington, antihistamine, anti-motion, Apoptosis, piperazine, sickness

Compound Identifiers

PubChem CID

64713