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Submit ReviewTetrabenazine
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)
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 |
| InChI Key | MKJIEFSOBYUXJB-HOCLYGCPSA-N |
| Smiles | O=C3[C@@H](CC(C)C)CN2CCC1=CC(OC)=C(OC)C=C1[C@@]([H])2C3 |
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 | |
|---|---|---|---|
| Solubility | |||
| ethanol | 9.52 | 30 | |
| 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.
| 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
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
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Reviews for Tetrabenazine
Average Rating: 5 (Based on 1 Review.)
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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).
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