Meclizine dihydrochloride

Biological Activity

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.

Technical Data

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.

Background References

1. The major role of peripheral release of histamine and 5-hydroxytryptamine in formalin-induced nociception.
   Parada et al.
   Neuroscience, 2001;102:937
2. Meclizine is neuroprotective in models of Huntington's disease.
   Gohil et al.
   Hum.Mol.Genet., 2010;20:294
3. Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor.
   Lau et al.
   J.Pharmacol.Exp.Ther., 2011;336:816

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