产品名称

丁苯那嗪(Tetrabenazine)

一般描述

Tetrabenazine is a drug formerly used as an antipsychotic and treatment of various movement disorders.

别 称

9,10-Dimethoxy-1,3,4,6,7,11b-hexahydro-3-isobutyl-2H-benzo[a]quinolizin-2-one;Nitoman;   Xenazine

纯 度

≥98.0%(HPLC)

CAS NO.

58-46-8

分子式

C¹⁹H²⁷NO³

分子量

317.428

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥30mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Tetrabenazine is a potent, selective inhibitor of the monoamine transporter 2 that causes a depletion of neuroactive peptides in nerve terminals and is used to treat chorea associated with Huntington disease. Tetrabenazine has not been associated with serum enzyme elevations during therapy or ed to instances of clinically apparent liver injury.

Tetrabenazine is hepatically metabolized. Carbonyl reductase in the liver is responsible for the formation of two major active metabolites: α-dihydrotetrabenazine (α-HTBZ) and β-dihydrotetrabenazine (β-HTBZ). α-HTBZ is further metabolized into 9-desmethyl-α-DHTBZ, a minor metabolite by CYP2D6 and with some contribution of CYP1A2. β-HTBZ is metabolized to another major circulating metabolite, 9-desmethyl-β-DHTBZ, by CYP2D6. The Tmax of this metabolite is 2 hours post-administration of tetrabenazine.

Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor (Ki =100 nM). It acts within the basal ganglia and promotes depletion of monoamine   neurotransmitters serotonin, norepinephrine, and dopamine from stores. It also decreases uptake into synaptic vesicles. Dopamine is required for fine motor movement, so the inhibition of its transmission is efficacious for hyperkinetic movement. Tetrabenazine exhibits weak in vitro binding affinity at the dopamine D2 receptor (Ki = 2100 nM).

l  包装与存储

包 装

50mg; 250mg; 1g

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov