(+) -Tetrabenazine [CAS 1026016-83-0]

(+) -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]

[1026016-83-0]

C19H27NO3

317.42

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

Monoamine Transporter

98.72

DMSO : 16.67 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature

H315, H319, H320

H315, H319, H320