| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Tetrabenazine (Ro 1-9569; trade name: Nitoman and Xenazin), a VMAT-inhibitor, is an FDA approved drug for the treatment of symptomatic treatment of hyperkinetic movement disorder. FDA approved the use of tetrabenazine to treat chorea associated with Huntington's disease (HD) On August 15, 2008, which is the first in the US. The precise mechanism of action of tetrabenazine is unknown. The antichorea effect is believed to be related to its effect as a reversible depletory of monoamines (such as dopamine, serotonin, norepinephrine and histamine)from nerve terminals)
| ln Vivo |
Adult male mice's levels of neurotransmitter molecules NE, DA, and 5-HT can be dose-dependently decreased by tetrabenazine (subcutaneous injection, 1~10 mg/kg, once) [1]. In male ICR mice, tetrabenazine (intraperitoneal injection, 0–2 mg/kg, once) selectively affects locomotion and can greatly reduce morphine-induced hyperactivity, although it also causes oral tremors and stereotyped behaviors [2]. Adult male Sprague-Dawley rats' tremor jaw movement (TJM) is dose-dependently increased by tetrabenazine (ip, 0.25-2 mg/kg, once weekly) [3].
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| Animal Protocol |
Animal/Disease Models: Adult male MAO A KO or 1-2 month old wide-type mice [1]
Doses: 1-10 mg/kg Route of Administration: subcutaneous injection; one-time Experimental Results:complete elimination of aggressive behavior at a concentration of 5 mg/kg, and Dramatically diminished their NE, DA and 5-HT levels. Animal/Disease Models: Male ICR mice (10 weeks old) [2] Doses: 0-2 mg/kg Route of Administration: intraperitoneal (ip) injection; Experimental Results: Pretreatment with tetrabenazine diminished morphine-induced hyperactivity. The METH-induced increase in locomotion was diminished at the 1 mg/kg dose. Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rats, body weight 350-450 g[3] Doses: 0.25-2 mg/kg Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. Weekly Experimental Results: Dramatically induced jaw tremor (TJM) at 2 mg/kg, with more motor injuries seen at higher doses (e.g. 3-4 mg/kg). |
| References |
[1]. J C Shih, et al. Ketanserin and tetrabenazine abolish aggression in mice lacking monoamine oxidase A. Brain Res. 1999 Jul 24;835(2):104-12.
[2]. Nobue Kitanaka, et al. Tetrabenazine, a vesicular monoamine transporter-2 inhibitor, attenuates morphine-induced hyperlocomotion in mice through alteration of dopamine and 5-hydroxytryptamine turnover in the cerebral cortex. Pharmacol Biochem Behav. 2018 [3]. S J Podurgiel, et al. The vesicular monoamine transporter (VMAT-2) inhibitor tetrabenazine induces tremulous jaw movements in rodents: implications for pharmacological models of parkinsonian tremor. Neuroscience. 2013 Oct 10;250:507-19. doi: 10.1016/j.neu [4]. Kenney, C., C. Hunter, and J. Jankovic, Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders. Mov Disord, 2007. 22(2): p. 193-7. [5]. Jankovic, J. and J. Beach, Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology, 1997. 48(2): p. 358-62. [6]. Ondo, W.G., P.A. Hanna, and J. Jankovic, Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol. Am J Psychiatry, 1999. 156(8): p. 1279-81. |
| Molecular Formula |
C19H27NO3
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|---|---|
| Molecular Weight |
317.42
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| CAS # |
58-46-8
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| Related CAS # |
Tetrabenazine Racemate;718635-93-9;(+)-Tetrabenazine;1026016-83-0;Tetrabenazine-d6;1392826-25-3;Tetrabenazine mesylate;804-53-5;(+)-Tetrabenazine-d6;1977511-05-9
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| SMILES |
O=C1[C@@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@]2([H])C1
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| InChi Key |
MKJIEFSOBYUXJB-HOCLYGCPSA-N
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| InChi Code |
InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3/t14-,16-/m0/s1
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| Chemical Name |
(3S,11bS)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one
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| Synonyms |
Tetrabenazine; trade names Nitoman and Xenazin; Ro 1 9569; Ro-1 9569; Ro 1-9569
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1504 mL | 15.7520 mL | 31.5040 mL | |
| 5 mM | 0.6301 mL | 3.1504 mL | 6.3008 mL | |
| 10 mM | 0.3150 mL | 1.5752 mL | 3.1504 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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