Meclizine (dihydrochloride monohydrate)

Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease^[1][2][3]. In Vitro: Meclizine (Meclozine; 50 µM; 24 hours) dihydrochloride monohydrate significantly increases cell survival in STHdh^Q111/111 cells at 24 h after the removal of serum, evidently by suppressing apoptosis, based on caspase 3 and 7 cleavage. The rescue is dose-dependent with an EC₅₀ of 17.3 µm, and a maximum efficacy of 218% increased survival over vehicle. Meclizine dihydrochloride monohydrate protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdh^Q111/111) and wild-type (STHdh^Q7/7) striatal cells^[2]. In Vivo: Meclizine (Meclozine; 10-100 mg/kg; ip) dihydrochloride monohydrate protects mouse against kidney ischemia. Pretreatment with 100 mg/kg of Meclizine, 17 or 24 h prior to ischemia shows kidney protection in mice. Meclizine dihydrochloride monohydrate reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis^[4].