(+) -Tetrabenazine

(+) -Tetrabenazine ((+) -TBZ; (3R,11bR) -TBZ; (3R,11bR) -Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1. target: VMAT-2 In vitro: (+) -Tetrabenazine inhibit the activity of the transporter but appear to interact differently with the protein. [2] (+) -Tetrabenazine inhibits reserpine binding to the transporter, suggesting that the sites may interact in an allosteric manner. [1] In vivo: 0.9% saline (80%) and dimethylsulfoxide (DMSO) (20%) . (+) -Tetrabenazine blocks dopamine (DA) storage and depletes striatal DA; (+) -Tetrabenazine was shown to induce tremulous jaw movements (TJMs) in rats and mice. The reference dose for administration is 2.0 mg/kg.[2]

Product Specifications

CAS Number

[1026016-83-0]

Product Name Alternative

(+) -TBZ; (3R,11bR) -TBZ; (3R,11bR) -Tetrabenazine

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Monoamine Transporter

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Purity

98.72

Solubility

DMSO : 16.67 mg/mL (ultrasonic)

Smiles

COC1=C(OC)C=C(CCN(C[C@H]2CC(C)C)[C@]3([H])CC2=O)C3=C1

Molecular Formula

C19H27NO3

Molecular Weight

317.42

Precautions

H315, H319, H320

References & Citations

[1]Podurgiel SJ et al. The MAO-B inhibitor deprenyl reduces the oral tremor and the dopamine depletion induced by the VMAT-2 inhibitor tetrabenazine. Behav Brain Res. 2016 Feb 1;298 (Pt B) :188-91.|[2]Peter D et al. Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetrabenazine. J Biol Chem. 1996 Feb 9;271 (6) :2979-86.