Tetrabenazine

Catalog # Availability Size / Price Qty
2175/10
2175/50
Vesicular Monoamine Transporter Inhibitors Small Molecule
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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%

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Biological Activity

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.

Technical Data

M.Wt:
317.2
Formula:
C19H27NO3
Solubility:
Soluble to 30 mM in ethanol and to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
58-46-8

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.

Additional Information

Other Product-Specific Information:

Background References

  1. Tetrabenazine, an amine-depleting drug, also blocks DA receptors in rat brain.
    Reches et al.
    J.Pharmacol.Exp.Ther, 1983;225:515
  2. Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants.
    Pettibone et al.
    Eur.J.Pharmacol., 1984;102:425
  3. Characterisation of the monoamine carrier of chromaffin granule membrane by binding of [2-3H]dihydrotetrabenazine.
    Scherman et al.
    Proc.Natl.Acad.Sci.USA, 1983;80:584
  4. Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetraben.
    Peter et al.
    J.Biol.Chem., 1996;271:2979

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