Catalog No.S1986 Synonyms: NSC 28728
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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|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.|
Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects.  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. 
|In vivo||Meclizine administration to mice increases expression of CAR target genes in a CAR-dependent manner.  Meclizine silence oxidative metabolism, suppresses apoptotic cell death in a murine cellular model of polyglutamine (polyQ) toxicity. |
|In vitro||DMSO||4 mg/mL warmed (8.62 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+95% Corn oil
For best results, use promptly after mixing.
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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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