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(+)-Tetrabenazine

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Chemical Structure| 1026016-83-0 同义名 : (+)-四苯那嗪 ;(+)-TBZ;(3R,11bR)-TBZ;(3R,11bR)-Tetrabenazine
CAS号 : 1026016-83-0
货号 : A651692
分子式 : C19H27NO3
纯度 : 95%
分子量 : 317.423
MDL号 : MFCD08461052
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(50.41 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
动物实验配方：
生物活性
描述 Vesicular monoamine transporter 2 (VMAT2) is a transmembrane protein that regulates the packaging and subsequent release of monoamine neurotransmitter molecules from neuronal vesicles into synapses. Tetrabenazine is a reversible inhibitor of VMAT2 that inhibits [3H]serotonin transport by VMAT2 with an IC50 value of ~300nM[3]. Injection of tetrabenazine at a dosage of 2.0mg/kg induced tremulous jaw movements in rats, while this effect was significantly attenuated by deprenyl, a monoamine oxidase type B inhibitor. Tetrabenazine at 2.0 mg/kg also had a biphasic effect on striatal extracellular dopamine in rats, which resulted in a remarkable increase (100%) in extracellular dopamine 30 minutes after injection, followed by a significant reduction (50%) after 90 minutes[4].
实验方案
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
参考文献

[1]Podurgiel SJ, Yohn SE, et al. The MAO-B inhibitor deprenyl reduces the oral tremor and the dopamine depletion induced by the VMAT-2 inhibitor tetrabenazine. Behav Brain Res. 2016 Feb 1;298(Pt B):188-91.

[2]Peter D, Vu T, et al. Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetrabenazine. J Biol Chem. 1996 Feb 9;271(6):2979-86.

[3]Peter D, Vu T, Edwards RH. Chimeric vesicular monoamine transporters identify structural domains that influence substrate affinity and sensitivity to tetrabenazine. J Biol Chem. 1996;271(6):2979-2986.

[4]Podurgiel SJ, Yohn SE, Dortche K, Correa M, Salamone JD. The MAO-B inhibitor deprenyl reduces the oral tremor and the dopamine depletion induced by the VMAT-2 inhibitor tetrabenazine. Behav Brain Res. 2016;298(Pt B):188-191.