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/ Tetrabenazine

丁苯那嗪 /Tetrabenazine {[allProObj[0].p_purity_real_show]}

货号：A769041 同义名： Ro 1-9569;NSC 169886

Tetrabenazine是一种VMAT抑制剂，用于治疗运动过度障碍（如亢进运动障碍）。

Tetrabenazine 化学结构 CAS号：58-46-8
Tetrabenazine 化学结构
CAS号：58-46-8
Tetrabenazine 3D分子结构
CAS号：58-46-8
Tetrabenazine 化学结构 CAS号：58-46-8
Tetrabenazine 3D分子结构 CAS号：58-46-8
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Tetrabenazine 纯度/质量文件 产品仅供科研

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Tetrabenazine 生物活性

描述 Tetrabenazine (TBZ; Xenazine) is a potent, selective, reversible depletor of monoamines from nerve terminals. TBZ inhibits the vesicular monoamine transporter type 2 which, in humans, is expressed nearly exclusively in the brain. TBZ is rapidly metabolized in the liver by carbonyl reductase to stereoisomers of hydrotetrabenazine, some of which are potent inhibitors of vesicular monoamine transporter type 2[3]. Tetrabenazine, a monoamine depleter and dopamine receptor blocker, is a VMAT-inhibitor used for treatment of hyperkinetic movement disorder[4]. Tetrabenazine (TBZ) depletes presynaptic dopamine in the CNS. TBZ is most effective in reducing chorea (including Huntington's disease associated chorea), tic associated with Tourette's syndrome and tardive dyskinesias[5]. TBZ selectively depletes central monoamines by reversibly binding to the type 2 vesicular monoamine transporter. TBZ, at adjusted dosages of up to 100 mg/day, effectively lessens chorea in ambulatory patients with Huntington disease[6]. Optimized nanoemulsion formulation of a tetrabenazine was robust and its delivery through nasal route is a viable alternative to other routes of administration for treatment of hyperkinesia associated with Huntington's disease[7].

Tetrabenazine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01734733 Parkinson's Disease Phase 1 Phase 2 Active, not recruiting April 29, 2019 New Zealand ... 展开 >> Auckland City Hospital Auckland, New Zealand 收起 <<
NCT01910480 Effect of Ketoconazole on the ... 展开 >>PK of NBI-98854 in Healthy Subjects 收起 << Phase 1 Completed - United States, Arizona ... 展开 >> Celerion Tempe, Arizona, United States, 85283 收起 <<
NCT02191358 - Completed - United States, California ... 展开 >> Dr. Michael Dao Garden Grove, California, United States, 92844 United States, Colorado Kaiser Permanente Colorado Denver, Colorado, United States, 80011 United States, Kentucky Gill Heart Institute Lexington, Kentucky, United States, 40508 United States, Maryland IRC Clinics Towson, Maryland, United States, 21204 United States, Massachusetts Internal Medicine & Cardiology Associates Fall River, Massachusetts, United States, 02720 Prima CARE Fall River, Massachusetts, United States, 02720 United States, Virginia Carilion Clinic Christiansburg, Virginia, United States, 24073 收起 <<

Tetrabenazine 参考文献

[1]Kenney C, Hunter C, et al. Long-term tolerability of tetrabenazine in the treatment of hyperkinetic movement disorders. Mov Disord. 2007 Jan 15;22(2):193-7.

[2]Jankovic J, Beach J. Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology. 1997 Feb;48(2):358-62.

[3]Jankovic J, Clarence-Smith K. Tetrabenazine for the treatment of chorea and other hyperkinetic movement disorders. Expert Rev Neurother. 2011 Nov;11(11):1509-23

[4]Ondo WG, Hanna PA, Jankovic J. Tetrabenazine treatment for tardive dyskinesia: assessment by randomized videotape protocol. Am J Psychiatry. 1999 Aug;156(8):1279-81

[5]Fasano A, Bentivoglio AR. Tetrabenazine. Expert Opin Pharmacother. 2009 Dec;10(17):2883-96

[6]Huntington Study Group. Tetrabenazine as antichorea therapy in Huntington disease: a randomized controlled trial. Neurology. 2006 Feb 14;66(3):366-72

[7]Arora A, Kumar S, Ali J, Baboota S. Intranasal delivery of tetrabenazine nanoemulsion via olfactory region for better treatment of hyperkinetic movement associated with Huntington's disease: Pharmacokinetic and brain delivery study. Chem Phys Lipids. 2020 Aug;230:104917

Tetrabenazine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.75mL

3.15mL

1.58mL

31.50mL

6.30mL

3.15mL

Tetrabenazine 技术信息

CAS号58-46-8
分子式C19H27NO3
分子量 317.423
别名 Ro 1-9569;NSC 169886;trade names Nitoman and Xenazin;TBZ;NSC 172187;Xenazine
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 35 mg/mL(110.26 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

Tags: Tetrabenazine | 58-46-8 | Ro 1-9569 | Monoamine Transporter | VMAT2 Inhibitor | Membrane Transporter/Ion Channel | Monoamine Transporter | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tetrabenazine 纯度/质量文件 | Tetrabenazine 生物活性 | Tetrabenazine 临床数据 | Tetrabenazine 参考文献 | Tetrabenazine 实验方案 | Tetrabenazine 技术信息

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