Background:

Meclizine dihydrochloride is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR.

Meclizine dihydrochloride is a histamine H1 receptor antagonist used to treat nausea and motion sickness, possesses anticholinergic, central nervous system depressant, and local anesthetic effects[1]. Meclizine dihydrochloride 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 (dihydrochloride) 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[2].

参考文献:
[1]. King, C.T., S.A. Weaver, and S.A. Narrod, Antihistamines and Teratogenicity in the Rat. J Pharmacol Exp Ther, 1965. 147: p. 391-8.
[2]. Huang, W., et al., Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR. Mol Endocrinol, 2004. 18(10): p. 2402-8.
[3]. Wendong Huang, et al. Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR