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(+)-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]
| Molecular Weight | 317.42 |
| Formula | C19H27NO3 |
| CAS Number | 1026016-83-0 |
| Form | Solid |
| Solubility (25°C) | DMSO 16.67 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Hassaan H Bashir, et al. Neurol Clin. Treatment of Tardive Dyskinesia
[4] Alfonso Fasano, et al. Expert Opin Pharmacother. Tetrabenazine
[5] Michael R Hayden, et al. Nat Rev Drug Discov. Tetrabenazine
| Related Monoamine Transporter Products |
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Tetrabenazine (Ro 1-9569) is a compound for the symptomatic treatment of hyperkinetic movement disorder. |
| Valbenazine
Valbenazine (NBI-98854) is a vesicular monoamine transporter-2 (VMAT2) inhibitor with a Ki of 110-190 nM. |
| 13-Hydroxyisobakuchiol
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol) is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). |
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