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Submit ReviewTetrabenazine
说明： Potent inhibitor of vesicular monoamine transport
化学名： (3R,11bR)-rel-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-one
纯度： ≥98% (HPLC)
生物活性 for Tetrabenazine
Tetrabenazine is an inhibitor of vesicular monoamine transport with a 10-fold selectivity for the VMAT2 transporter over VMAT1 (IC50 values = 0.3 μM and 3.4 μM, respectively). Tetrabenazine blocks D2 receptors and dopamine uptake (IC50 = 0.12 μM) and inhibits serotonin transport by VMAT2 (IC50 = 300 nM). In an animal model of Huntington's disease, Tetrabenazine prevents the decline in motor control and reduces loss of striatal neurons. Tetrabenazine increases cFos expression in the thalamus and hippocampus, reduces brain connectivity and spontaneous locomotion and also causes behavioral depression.
化合物库 for Tetrabenazine
Tetrabenazine is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Tetrabenazine
| 分子量 | 317.2 |
| 公式 | C19H27NO3 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 58-46-8 |
| PubChem ID | 11634155 |
| InChI Key | LGKOWFOTKBOLFX-QNQDLDTESA-N |
| Smiles | O=C1[C@@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@]2([H])C1.O=C4[C@H](CC(C)C)CN5CCC6=CC(OC)=C(OC)C=C6[C@@]5([H])C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Tetrabenazine
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.74 | 100 |
制备储备液 for Tetrabenazine
以下数据基于产品分子量 317.2。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.15 mL | 15.76 mL | 31.53 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.31 mL |
| 10 mM | 0.32 mL | 1.58 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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产品说明书 for Tetrabenazine
参考文献 for Tetrabenazine
参考文献是支持产品生物活性的出版物。
Reches et al (1983) Tetrabenazine, an amine-depleting drug, also blocks DA receptors in rat brain. J.Pharmacol.Exp.Ther 225 515 PMID: 6864517
Pettibone et al (1984) Tetrabenazine-induced depletion of brain monoamines: characterisation and interaction with selected antidepressants. Eur.J.Pharmacol. 102 425 PMID: 6489435
Peter et al (1996) Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetraben. J.Biol.Chem. 271 2979 PMID: 8621690
Scherman et al (1983) Characterisation of the monoamine carrier of chromaffin granule membrane by binding of [2-3H]dihydrotetrabenazine. Proc.Natl.Acad.Sci.USA 80 584
Cruces-Solis et al (2020) Whole-brain signatures of functional connectivity after bidirectional modulation of the dopaminergic system in mice. Neuropharmacology 178 108246 PMID: 32771528
If you know of a relevant reference for Tetrabenazine, please let us know.
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关键词: Tetrabenazine, Tetrabenazine supplier, Potent, inhibitors, inhibits, vesicular, monoamine, transport, depletes, noradrenalin, stores, dopamine, 5-HT, Noradrenalin, Transporter, NET, Adrenergic, Transporters, Monoamine, Neurotransmitter, DAT, Dopamine, Serotonin, SERT, reuptake, 5-Hydroxytryptamine, noradrenaline, hunt, Vesicular, 2175, Tocris Bioscience
篇 Tetrabenazine 的引用文献
引用文献是使用了 Tocris 产品的出版物。
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Tetrabenazine 的评论
平均评分: 5 (Based on 1 Review.)
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Depletion of dopamine stores.
By
Sergiy Sylantyev on 10/15/2020
种属： Human
细胞系/组织： Stem cell - derived neurons
Tetrabenazine (TBZ) was used to deplete dopamine stores in cultured dopamine neurons and thus counteract dopamine-generated allosteric antagonism at NMDA receptors. 20-minute incubation of cell culture in 1 µM tetrabenazine had led to significant amplitude increase of NMDA-receptor – generated series of evoked post-synaptic potentials (see illustration).
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.