Tetrabenazine

Product Description

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.

Solubility

Preparing Stock Solutions for Tetrabenazine

The following data is based on the product molecular weight 317.20

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.15 mL	15.76 mL	31.53 mL
5 mM	0.63 mL	3.15 mL	6.31 mL
10 mM	0.32 mL	1.58 mL	3.15 mL
50 mM	0.06 mL	0.32 mL	0.63 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Cruces-Solis Whole-brain signatures of functional connectivity after bidirectional modulation of the dopaminergic system in mice. Neuropharmacology 2020 PMID: 32771528
• Scherman Characterisation of the monoamine carrier of chromaffin granule membrane by binding of [2-³H]dihydrotetrabenazine. Proc.Natl.Acad.Sci.USA
• Pettibone Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants. Eur.J.Pharmacol. 1984 PMID: 6489435
• Peter Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetraben. J.Biol.Chem. 1996 PMID: 8621690
• Reches Tetrabenazine, an amine-depleting drug, also blocks DA receptors in rat brain. J.Pharmacol.Exp.Ther 1983 PMID: 6864517