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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.
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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
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Keywords: Tetrabenazine, Tetrabenazine supplier, Potent, inhibitors, inhibits, vesicular, monoamine, transport, depletes, noradrenalin, stores, dopamine, 5-HT, Noradrenalin, Transporter, NET, Adrenergic, Transporters, Monoamine, Neurotransmitter, DAT, Dopamine, Serotonin, SERT, reuptake, 5-Hydroxytryptamine, noradrenaline, hunt, Vesicular, 2175, Tocris Bioscience
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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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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 (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.