Pricing Availability   Qty
Description: Potent inhibitor of vesicular monoamine transport
Chemical Name: (3R,11bR)-rel-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-one
Purity: ≥98% (HPLC)
Reviews (1)
Literature (2)

Biological Activity for Tetrabenazine

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.

Compound Libraries for Tetrabenazine

Tetrabenazine is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Tetrabenazine

M. Wt 317.2
Formula C19H27NO3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 58-46-8
PubChem ID 11634155
Smiles O=C1[C@@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@]2([H])C1.O=C4[C@H](CC(C)C)CN5CCC6=CC(OC)=C(OC)C=C6[C@@]5([H])C4

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.

Solubility Data for Tetrabenazine

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 31.74 100

Preparing Stock Solutions for Tetrabenazine

The following data is based on the product molecular weight 317.2. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

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Product Datasheets for Tetrabenazine

Certificate of Analysis / Product Datasheet
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References for Tetrabenazine

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

Reches et al (1983) Tetrabenazine, an amine-depleting drug, also blocks DA receptors in rat brain. J.Pharmacol.Exp.Ther 225 515 PMID: 6864517

Pettibone et al (1984) Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants. Eur.J.Pharmacol. 102 425 PMID: 6489435

Peter et al (1996) Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetraben. J.Biol.Chem. 271 2979 PMID: 8621690

Scherman et al (1983) Characterisation of the monoamine carrier of chromaffin granule membrane by binding of [2-3H]dihydrotetrabenazine. Proc.Natl.Acad.Sci.USA 80 584

Cruces-Solis et al (2020) Whole-brain signatures of functional connectivity after bidirectional modulation of the dopaminergic system in mice. Neuropharmacology 178 108246 PMID: 32771528

If you know of a relevant reference for Tetrabenazine, please let us know.

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Citations for Tetrabenazine

Citations are publications that use Tocris products.

Currently there are no citations for Tetrabenazine. Do you know of a great paper that uses Tetrabenazine from Tocris? Please let us know.

Reviews for Tetrabenazine

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Depletion of dopamine stores.
By Sergiy Sylantyev on 10/15/2020
Species: Human
Cell Line/Tissue: Stem cell - derived neurons

Tetrabenazine (TBZ) was used to deplete dopamine stores in cultured dopamine neurons and thus counteract dopamine-generated allosteric antagonism at NMDA receptors. 20-minute incubation of cell culture in 1 µM tetrabenazine had led to significant amplitude increase of NMDA-receptor – generated series of evoked post-synaptic potentials (see illustration).

review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Dopamine Receptors Scientific Review

Dopamine Receptors Scientific Review

Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.

Parkinson's Disease Poster

Parkinson's Disease Poster

Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.