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Category:
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Transporters Neurotransmitter TransportersDopamine Transporters
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Cat.No.
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Product Name
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2175 |
Tetrabenazine
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Price and Availability
Click here for full price details of
Tetrabenazine
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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 |
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Biological Activity:
Potent
inhibitor of vesicular monoamine uptake; depletes stores of dopamine, serotonin
and noradrenaline. 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 behavioural depression; inhibits locomotor activity and
produces hypothermia upon systemic administration in rats and mice.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Reches et al (1983) Tetrabenazine,
an amine-depleting drug, also blocks dopamine receptors in rat brain.
J.Pharmacol.Exp.Ther 225 515. 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. Pettibone et al (1984) Tetrabenazine-induced depletion of
brain monoamines: characterisation and interaction with selected
antidepressants. Eur.J.Pharmacol. 102 425. Peter et al
(1996) Chimeric vesicular monoamine transporters identify structural domains
that influence substrate affinity and sensitivity to tetrabenazine.
J.Biol.Chem. 271 2979.
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or by Research Area
Keywords: Tetrabenazine, Neurotransmitter Transporters, Potent Inhibitor Of Vesicular Monoamine Transport; Depletes Dopamine Stores, Tocris Bioscience
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Product Feature
Uptake Inhibitors
Key Uptake Inhibitors now available from Tocris include:
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