Meclizine

Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine 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) significantly increases cell survival in STHdh 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 protects striatal cells expressing polyglutamine (polyQ)-expanded huntingtin from serum withdrawal-induced apoptosis of mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells^[2]. In Vivo: Meclizine (Meclozine; 10-100 mg/kg; ip) 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 reduces mitochondrial oxygen consumption by directly inhibiting the Kennedy pathway of phosphatidylethanolamine biosynthesis and up-regulated glycolysis^[4].