Tetrabenazine-d7 is intended for use as an internal standard for the quantification of tetrabenazine by GC- or LC-MS. Tetrabenazine is an inhibitor of vesicular monoamine transporter 2 (VMAT2) that is selective over VMAT1 (Kis = 97 and >20,000 nM, respectively, in a serotonin uptake assay).1 It dose-dependently reduces levels of the monoamines norepinephrine , dopamine , and serotonin in rat brain and has been used to induce depressive-like behavior in animal models.2,3 Tetrabenazine (5 mg/kg) improves performance in balance beam and rotarod tests and prevents decreases in the number of striatal medium spiny neurons (MSNs) in a YAC128 transgenic mouse model of Huntington's disease.4 Formulations containing tetrabenazine have been used in the treatment of chorea associated with Huntington's disease.
1.Erickson, J.D., SchÄfer, M.K.H., Bonner, T.I., et al.Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporterProc. Natl. Acad. Sci. U.S.A.93(10)5166-5171(1996) 2.Pettibone, D.J., Totaro, J.A., and Pflueger, A.B.Tetrabenazine-induced depletion of brain monoamines: Characterization and interaction with selected antidepressantsEur. J. Pharmacol.102(3-4)425-430(1984) 3.Preskorn, S.H., Kent, T.A., Glotzbach, R.K., et al.Cerebromicrocirculatory defects in animal model of depressionPsychoparmacology (Berl).84(2)196-199(1984) 4.Wang, H., Chen, X., Li, Y., et al.Tetrabenazine is neuroprotective in Huntington's disease miceMol. Neurodegener.5:18(2010)