Binding of alpha-dihydrotetrabenazine to the vesicular monoamine transporter is stereospecific.
(1995) European Journal of Pharmacology — Vol. 278, n° 3, p. 249-252 (1995)
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- Abstract
- The two enantiomers of alpha-dihydrotetrabenazine were separated using chiral high performance liquid chromatography. The (+)-isomer showed high affinity in vitro (Ki = 0.97 +/- 0.48 nM) for the vesicular monoamine transporter (VMAT2) in rat brain striatum, whereas the (-)-isomer was inactive (Ki = 2.2 +/- 0.3 microM). Each isomer was then synthesized in carbon-11 labeled form, and regional brain biodistributions in mice determined after intravenous injection. Only (+)-alpha-dihydrotetrabenazine showed selective and specific accumulations in regions of dense monoaminergic innervation (e.g., striatum, hypothalamus), which could be blocked by coinjection of unlabeled tetrabenazine. Binding of alpha-dihydrotetrabenazine to the vesicular monoamine transporter is thus stereospecific.
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Kilbourn, M., Lee, L., Vander Borght, T., Jewett, D., & Frey, K. (1995). Binding of alpha-dihydrotetrabenazine to the vesicular monoamine transporter is stereospecific. European Journal of Pharmacology, 278(3), 249-252. https://hdl.handle.net/2078.5/162364 (Original work published 1995)