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 ActivityPotent 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Tetrabenazine, an amine-depleting drug, also blocks DA receptors in rat brain.
Reches et al.
Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants.
Pettibone et al.
Characterisation of the monoamine carrier of chromaffin granule membrane by binding of [2-3H]dihydrotetrabenazine.
Scherman et al.
Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetraben.
Peter et al.
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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).