产品说明书
Tetrabenazine
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同义名 : | Ro 1-9569;NSC 169886;trade names Nitoman and Xenazin;TBZ;NSC 172187;Xenazine |
| CAS号 : | 58-46-8 | |
| 货号 : | A769041 | |
| 分子式 : | C19H27NO3 | |
| 纯度 : | 98% | |
| 分子量 : | 317.423 | |
| MDL号 : | MFCD00042740 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
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 |
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| 动物实验配方： |
| 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]. | ||
| 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 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.32mL |
15.75mL 3.15mL 1.58mL |
31.50mL 6.30mL 3.15mL |
| 参考文献 |
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[5]Fasano A, Bentivoglio AR. Tetrabenazine. Expert Opin Pharmacother. 2009 Dec;10(17):2883-96 |