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1104-22-9 (Meclizine (dihydrochloride))

1

Identification

Meclizine (dihydrochloride) Meclizine (dihydrochloride)
Name Meclizine (dihydrochloride)
Formula C25H29Cl3N2
MW 463.87
CAS No. 1104-22-9
EINECS 214-164-8
Smiles ClC1=CC=C(C=C1)C(C2=CC=CC=C2)N3CCN(CC4=CC=CC(C)=C4)CC3.Cl.Cl
Synonyms 1-[(4-Chlorophenyl)-phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine dihydrochloride; 1-((4-chlorophenyl)(phenyl)methyl)-4-(3-methylbenzyl)piperazine dihydrochloride
InChI InChI=1S/C25H27ClN2.2ClH/c1-20-6-5-7-21(18-20)19-27-14-16-28(17-15-27)25(22-8-3-2-4-9-22)23-10-12-24(26)13-11-23;;/h2-13,18,25H,14-17,19H2,1H3;2*1H
2

Introduction

Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness Target: Histamine H1 Receptor 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].

Background Information

Meclizine is a human pregnane X receptor (hPXR) agonist. It possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Its antiemetic and antivertigo effects are not fully understood, but its central anticholinergic properties are partially responsible. ......by AdooQ BioScience, LLC
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 inv ......by BOC Sciences
Meclizine dihydrochloride is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. Meclizine hydrochloride increases human pregnane X receptor (hPXR) target gene expression in human hepatocyte primary cultures. ......by MedKoo Biosciences, Inc.
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. ......by Selleck Chemicals LLC
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. ......by Target Molecule Corp.
Human pregnane X receptor (hPXR) agonist; stronger activator of hPXR than rat PXR. Increases hPXR target gene expression in human hepatocyte primary cultures. Also acts as a histamine H1 receptor antagonist. Confers neuroprotection in models of polyQ toxicity. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines HepG2 cells
Conditions ~10 μM; 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.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Mouse
Dosage 100 mg/kg
Formulation corn oil
Administration i.p.
Source Selleck Chemicals LLC
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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000012515

Storage condition

Desiccate at RT by Tocris Bioscience Inc.

Solubility

DMSO 1 mg/mL; Water <1 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 1 mg/mL (2.15 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 5% DMSO+95% Corn oil10 mg/mL by Selleck Chemicals LLC
Soluble to 50 mM in DMSO by Tocris Bioscience Inc.
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Mechanism and Indication

Signaling Pathways Immunology/Inflammation GPCR/G Protein
Target Histamine Receptor
Research Area Neurological Disease
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Meclizine (dihydrochloride) - Launched
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Safety Data of Meclizine (dihydrochloride)

Hazard Symbols : Xn
Risk Statements : 22-63
Safety Statements : 22-36
RTECS : TL2005000
WGKGermany : 3
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
Ark Pharm, Inc. USA
Astatech, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 100mg/USD60();5g/USD96() USA
Cayman Chemical Company USA
D.K. Pharma Chem Pvt. Ltd. India
Hangzhou Neway Chemicals Co., Ltd. China
Huangshi Fuertai Chemical Co., Ltd. China
MedChemexpress Co., Ltd. 100mg/USD60();5g/USD96() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC 50mg/USD97(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 100mg/USD60();5g/USD96() China
Shanghai Licheng Chemical Co., Ltd. China
Target Molecule Corp. 2mg/USD20();10mg/USD42();50mg/USD86();200mg/USD122() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 1104-22-9

Name CAS No Formula MW
Meclozine 569-65-3 C25H28Cl2N2 427.41
Meclizine (dihydrochloride monohydrate) 31884-77-2 C25H31Cl3N2O 481.89

Recommended Compounds in Histamine Receptor

Name CAS No Formula MW
Doxylamine (succinate) 562-10-7 C21H28N2O5 388.46
Ebastine 90729-43-4 C32H39NO2 469.66
Azelastine 58581-89-8 C22H24ClN3O 381.9
Epinastine 80012-43-7 C16H15N3 249.31
Hydroxyzine (dihydrochloride) 2192-20-3 C21H29Cl3N2O2 447.83
Hydroxyzine 68-88-2 C21H27ClN2O2 374.9
Desloratadine 100643-71-8 C19H19ClN2 310.82
Pemirolast (potassium) 100299-08-9 C10H7KN6O 266.3
Betahistine (dihydrochloride) 5579-84-0 C8H14Cl2N2 209.12
Brompheniramine (maleate) 980-71-2 C20H23BrN2O4 435.31
Azelastine (hydrochloride) 79307-93-0 C22H25Cl2N3O 418.36
Olopatadine (hydrochloride) 140462-76-6 C21H24ClNO3 373.87
Famotidine 76824-35-6 C8H15N7O2S3 337.45
Nizatidine 76963-41-2 C12H21N5O2S2 331.46
Roxatidine (Acetate Hydrochloride) 93793-83-0 C19H29ClN2O4 384.9
Diphenhydramine (hydrochloride) 147-24-0 C17H22ClNO 291.82
Clemastine (fumarate) 14976-57-9 C25H30ClNO5 459.96
Chlorpheniramine (maleate) 113-92-8 C20H23ClN2O4 390.86
Ranitidine (hydrochloride) 66357-59-3 C13H23ClN4O3S 350.86
Mianserin (hydrochloride) 21535-47-7 C18H21ClN2 300.83

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

Meclizine (dihydrochloride)

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