Tetrabenazine

Cat. No. 2175

Tetrabenazine C19H27NO3 [58-46-8]

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Chemical Name: (3R,11bR)-rel-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-one

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.

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Peter et al (1996) Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetrabenazine. J.Biol.Chem. 271 2979. PMID: 8621690.

Pettibone et al (1984) Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants. Eur.J.Pharmacol. 102 425. PMID: 6489435.

Reches et al (1983) Tetrabenazine, an amine-depleting drug, also blocks dopamine receptors in rat brain. J.Pharmacol.Exp.Ther 225 515. PMID: 6864517.

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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