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Biological Activity for Tetrabenazine
Tetrabenazine is a potent inhibitor of vesicular monoamine uptake; depletes stores of dopamine, serotonin and noradrenalin. Binds with high affinity (IC50= 3.2 nM) to vesicular monoamine transporter (VMAT) in chromaffin granule membranes and displays higher affinity for VMAT2 than VMAT1. Also reported to block dopamine receptors. Causes behavioral depression; inhibits locomotor activity and produces hypothermia upon systemic administration in rats and mice.
Deuterated analog also available.
Compound Libraries for Tetrabenazine
Technical Data for Tetrabenazine
|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.
Solubility Data for Tetrabenazine
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
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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, Vesicular, 2175, Tocris Bioscience
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
Average Rating: 5 (Based on 1 Review.)
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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).
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
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.