Meclizine-d8 is intended for use as an internal standard for the quantification of meclizine by GC- or LC-MS. Meclizine is a histamine H1 receptor antagonist (Ki = 250 nM).1 Pretreatment with meclizine (2.5-30 mg/kg, i.p.) reduces ovalbumin-induced mast cell degranulation, edema, and leukocyte influx in rat lung.2 Formulations containing meclizine have been used in the treatment of motion sickness and vertigo.
1.Tran, V.T., Chang, R.S.L., and Snyder, S.H.Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramineProc. Natl. Acad. Sci. U.S.A.75(12)6290-6294(1978) 2.Pasquale, C.P., e Silva, P.M., Lima, M.C., et al.Suppression by cetirizine of pleurisy triggered by antigen in actively sensitized ratsEur. J. Pharmacol.223(1)9-14(1992)