Tetrabenazine

Name: Tetrabenazine
Brand: Tocris Bioscience
SKU: 2175
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 2175

(1)

Citations (18)

COA / SDS

Potent inhibitor of vesicular monoamine transport

Key Product Details

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)
Molecular Weight:	317.2

View Full Technical Details for Tetrabenazine

Technical Data
Citations / Reviews (1)

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	LGKOWFOTKBOLFX-QNQDLDTESA-N
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 for Tetrabenazine

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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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References for Tetrabenazine

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