テトラベナジン
Based on 1 publication(s) in Google Scholar
Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.95%
- CAS 番号: 58-46-8
- 分子式: C19H27NO3
- 分子量:317.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Tetrabenazine
MoreDopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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D2 Receptor ~2.1 μM (Ki) |
Tetrabenazine reversibly inhibits human VMAT2 with a Ki of ~100 nM, reducing monoamine uptake into synaptic vesicles and depleting presynaptic monoamine stores[1].
Tetrabenazine inhibits dopamine D2 receptors in striatal membranes with a Ki of ~2.1 μM[1].
Tetrabenazine (0.3-10.0 μg/mL; 4 h) releases serotonin from rabbit blood platelets in vitro in a concentration-dependent manner[3].
Tetrabenazine (5-20 mg/L) is 60% bound to nondiffusible components of rabbit plasma[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tetrabenazine (7 days) causes irreversible locomotor changes and substantia nigra pars compacta neuronal damage in healthy rats[1].
Tetrabenazine (50-150 mg/kg; i.v.; daily for 3-9 days) exhibits short-lived, central nervous system-selective Reserpine (HY-N0480)-like effects in rabbits[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand White male (~2 kg)[3]
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Dosage:50 mg/kg; 150 mg/kg
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Administration:i.v.; daily for 3, 7, 9 days
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Result:Decreased brain serotonin to ~50% of normal within 1 hour, remained at this level for several hours, and returned to near normal by 18-24 hours.
Declined brain norepinephrine to ~15% of normal over 4 hours, and returned to ~70% of normal by 24 hours.
Did not measurably affect peripheral serotonin in blood platelets and small intestine, and norepinephrine in heart.
Caused <10% depletion of adrenal catecholamines at 4 hours and ~40% depletion at 24 hours.
Reduced plasma drug levels to <3 μg/mL by 6 hours, and made them undetectable by 24 hours.
Reached brain drug levels of ~45 μg/g within 10 minutes, declined to ~1.3 μg/g by 6 hours, and made them undetectable by 24 hours.
Failed to affect intestinal/platelet serotonin or heart norepinephrine, but caused 50% depletion of adrenal catecholamines by the end of infusion with single 150 mg/kg i.v. dose.
Showed no drug accumulation in plasma or tissues 24 hours after the last dose with repeated 50 mg/kg daily i.v. doses.
化学情報
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CAS 番号 58-46-8
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性状 Solid
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分子量 317.43
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分子式 C19H27NO3
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Color White to off-white
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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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別名
Tetrabenazine; Ro 1-9569
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 25 mg/mL (78.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.33 mg/mL (10.49 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.33 mg/mL (10.49 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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参考文献
[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. [Content Brief]
[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 Sep;172:9-16. doi: 10.1016/j.pbb.2018.07.002. Epub 2018 Jul 12. [Content Brief]
[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.neuroscience.2013.07.008. Epub 2013 Jul 15. [Content Brief]
[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. [Content Brief]
[5]. Jankovic, J. and J. Beach, Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology, 1997. 48(2): p. 358-62. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1503 mL | 15.7515 mL | 31.5030 mL | 78.7575 mL |
| 5 mM | 0.6301 mL | 3.1503 mL | 6.3006 mL | 15.7515 mL | |
| 10 mM | 0.3150 mL | 1.5752 mL | 3.1503 mL | 7.8758 mL | |
| 15 mM | 0.2100 mL | 1.0501 mL | 2.1002 mL | 5.2505 mL | |
| 20 mM | 0.1575 mL | 0.7876 mL | 1.5752 mL | 3.9379 mL | |
| 25 mM | 0.1260 mL | 0.6301 mL | 1.2601 mL | 3.1503 mL | |
| 30 mM | 0.1050 mL | 0.5251 mL | 1.0501 mL | 2.6253 mL | |
| 40 mM | 0.0788 mL | 0.3938 mL | 0.7876 mL | 1.9689 mL | |
| 50 mM | 0.0630 mL | 0.3150 mL | 0.6301 mL | 1.5752 mL | |
| 60 mM | 0.0525 mL | 0.2625 mL | 0.5251 mL | 1.3126 mL |
Tetrabenazine 関連分類
HY-B0590 関連分類
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