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Submit ReviewMeclizine dihydrochloride
Description: Human pregnane X receptor agonist; H1 antagonist
Alternative Names: Meclozine
Chemical Name: 1-[(4-Chlorophenyl)phenylmethyl]4-[(3-methylphenyl)methyl]piperazine dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for Meclizine dihydrochloride
Meclizine dihydrochloride is a human pregnane X receptor (hPXR) agonist; it is a more potent activator of hPXR than rat PXR. Meclizine increases hPXR target gene expression in human hepatocyte primary cultures. It also acts as a histamine H1 receptor antagonist. Meclizine attenuates mitochondrial respiration and increases glycolysis. The product inhibits rotenone-induced cell death in stem cell-derived dopaminergic neuronal culture and confers neuroprotection in models of polyglutamine (polyQ) toxicity.
Compound Libraries for Meclizine dihydrochloride
Meclizine dihydrochloride is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Meclizine dihydrochloride
| M. Wt | 463.87 |
| Formula | C25H27ClN2.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1104-22-9 |
| PubChem ID | 64713 |
| InChI Key | VCTHNOIYJIXQLV-UHFFFAOYSA-N |
| Smiles | CC1=CC(CN(CC4)CCN4C(C3=CC=C(Cl)C=C3)C2=CC=CC=C2)=CC=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Meclizine dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.19 | 50 |
Preparing Stock Solutions for Meclizine dihydrochloride
The following data is based on the product molecular weight 463.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.31 mL | 21.56 mL | 43.12 mL |
| 2.5 mM | 0.86 mL | 4.31 mL | 8.62 mL |
| 5 mM | 0.43 mL | 2.16 mL | 4.31 mL |
| 25 mM | 0.09 mL | 0.43 mL | 0.86 mL |
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Product Datasheets for Meclizine dihydrochloride
References for Meclizine dihydrochloride
References are publications that support the biological activity of the product.
Parada et al (2001) The major role of peripheral release of histamine and 5-hydroxytryptamine in formalin-induced nociception. Neuroscience 102 937 PMID: 11182255
Gohil et al (2010) Meclizine is neuroprotective in models of Huntington's disease. Hum.Mol.Genet. 20 294 PMID: 20977989
Lau et al (2011) Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor. J.Pharmacol.Exp.Ther. 336 816 PMID: 21131266
Oosterveen et al (2021) Pluripotent stem cell derived dopaminergic subpopulations model the selective neuron degeneration in Parkinson's disease. Stem Cell Reports PMID: 34678205
If you know of a relevant reference for Meclizine dihydrochloride, please let us know.
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2 Citations for Meclizine dihydrochloride
Citations are publications that use Tocris products. Selected citations for Meclizine dihydrochloride include:
Oosterveen et al (2021) Pluripotent stem cell derived dopaminergic subpopulations model the selective neuron degeneration in Parkinson's disease. Stem Cell Reports 16 2718 PMID: 34678205
Hong et al (2016) Meclizine-induced enhanced glycolysis is neuroprotective in Parkinson disease cell models. Sci Rep 6 25344 PMID: 27145922
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Literature in this Area
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Retinoid Receptors Scientific Review
Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.