Meclizine-d₈ dihydrochloride  (Synonyms: Meclozine-d₈(dihydrochloride))

Meclizine-d₈ (dihydrochloride) is the deuterium labeled Meclizine dihydrochloride. Meclizine (Meclozine) dihydrochloride, 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 is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

471.92

C₂₅H₂₁D₈Cl₃N₂

1432062-16-2

固体

White to off-white

盐酸美克洛嗪 d₈ (双盐酸盐)

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness.

  [3]. Vishal M Gohil, et al. Meclizine is neuroprotective in models of Huntington's disease. Hum Mol Genet. 2011 Jan 15;20(2):294-300.  [Content Brief]

  [4]. Wendong Huang, et al. Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR  [Content Brief]

  [5]. Seiji Kishi, et al. Meclizine Preconditioning Protects the Kidney Against Ischemia-Reperfusion Injury. EBioMedicine. 2015 Jul 29;2(9):1090-101.  [Content Brief]