Tetrabenazine (Nitoman, Xenazine) is a compound for the symptomatic treatment of hyperkinetic movement disorder. Tetrabenazine works mainly as a VMAT-inhibitor and as such promotes the early metabolic degradation of monoamines, in particular the neurotransmitter dopamine.
| Molecular Weight | 317.42 |
| Formula | C19H27NO3 |
| CAS Number | 58-46-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Michael A Cummings, et al. Deuterium Tetrabenazine for Tardive Dyskinesia
[3] No authors listed. J Pharm Belg. Tetrabenazine (tetrabenazine Orphan) orally
| Related Monoamine Transporter Products |
|---|
| VMAT2-IN-2 tosylate
VMAT2-IN-2 tosylate is a potent VMAT2 inhibitor. |
| 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). |
| Tetrabenazine mesylate
Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease. |
| Tetrabenazine Racemate
Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). (1) The reference for administration is 0.25-0.75 mg/kg IP (2) Injections of tetrabenazine into accumbens core also reduced FR5 lever pressing and increased chow intake. (3) Tetrabenazine (Racemate) reduced extracellular DA and altered DARPP-32 signaling in both substance-P- and enkephalin-containing accumbens neurons. (4) Tetrabenazine (Racemate) inhibits locomotor activity and produces hypothermia upon systemic administration in rats and mice. |
| (+)-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] |
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