Tetrabenazine

Biological Activity

Tetrabenazine is an inhibitor of vesicular monoamine transport with a 10-fold selectivity for the VMAT2 transporter over VMAT1 (IC₅₀ values = 0.3 μM and 3.4 μM, respectively). Tetrabenazine blocks D₂ receptors and dopamine uptake (IC₅₀ = 0.12 μM) and inhibits serotonin transport by VMAT2 (IC₅₀ = 300 nM). In an animal model of Huntington's disease, Tetrabenazine prevents the decline in motor control and reduces loss of striatal neurons. Tetrabenazine increases cFos expression in the thalamus and hippocampus, reduces brain connectivity and spontaneous locomotion and also causes behavioral depression.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Tetrabenazine, an amine-depleting drug, also blocks DA receptors in rat brain.
   Reches et al.
   J.Pharmacol.Exp.Ther, 1983;225:515
2. Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants.
   Pettibone et al.
   Eur.J.Pharmacol., 1984;102:425
3. Characterisation of the monoamine carrier of chromaffin granule membrane by binding of [2-³H]dihydrotetrabenazine.
   Scherman et al.
   Proc.Natl.Acad.Sci.USA, 1983;80:584
4. Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetraben.
   Peter et al.
   J.Biol.Chem., 1996;271:2979

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