Synthesis of H-Labeled Tetrabenazine (TBZ).

Synthesis of H-Labeled Tetrabenazine (TBZ).
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DOI:
10.1002/jlcr.1881
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发表时间:
2011-06-15
影响因子:
1.8
通讯作者:
Tanga, Mary J.
Tanga, Mary J.
中科院分区:
医学4区
文献类型:
--
作者:
Rhee, Sung-Whi;Ryan, Kenneth J.;Tanga, Mary J.

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四苯喹嗪(TBZ)(1,3,4,6,7,11b-六氢-9,10-二甲氧基-3-(2-甲基丙基)-2H-苯并[a]喹啉-2-酮)是一种囊泡单胺转运蛋白2抑制剂,经氚标记后具有高比活度和放射化学纯度。利用末端双键的前体的催化氢化来引入氚。该方法提供了具有高比活度和放射化学纯度的氚标记的TBZ,这允许进一步研究TBZ在神经领域中的作用。
Tetrabenazine (TBZ) (1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolin-2-one), a vesicular monamine transporter 2 inhibitor, was prepared as a tritium-labeled compound with high specific activity and radiochemical purity. Catalytic hydrogenation of a precursor with the terminal double bond was used to introduce the tritium. This method provides tritium-labeled TBZ with high specific activity and radiochemical purity, which allow the further investigation of a TBZ in the neurological field.
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