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[一种丁苯那嗪衍生物与嗜铬粒细胞膜单胺转运体的结合]

[Binding of a tetrabenazine derivative to the monoamine transporter of the chromaffin granule membrane].

作者信息

Scherman D, Jaudon P, Henry J P

出版信息

C R Seances Acad Sci III. 1981 Oct 5;293(4):221-4.

PMID:6794869
Abstract

[2-3H] dihydrotetrabenazine (2-hydroxy-3-isobutyl-9-10-dimethoxy-1,2,3,4,6,7 hexahydro-11 bH-benzo [a] quinolizine), a derivative of tetrabenazine obtained by tritiated borohydride reduction, binds to the membrane of purified chromaffin granules. The binding equilibrium has been studied by filtration and by centrifugation of ligand-membrane complexes. Saturable binding sites (190 pmol/mg protein), characterized by a dissociation equilibrium constant KD = 90 nM have been described. The correlation existing between dihydrotetrabenazine site occupancy and noradrenaline uptake inhibition indicates that these sites are located on the monoamine transporter.

摘要

[2-³H]二氢丁苯那嗪(2-羟基-3-异丁基-9,10-二甲氧基-1,2,3,4,6,7-六氢-11bH-苯并[a]喹嗪)是通过氚化硼氢化还原得到的丁苯那嗪衍生物,可与纯化的嗜铬颗粒膜结合。已通过配体-膜复合物的过滤和离心研究了结合平衡。已描述了具有解离平衡常数KD = 90 nM的可饱和结合位点(190 pmol/mg蛋白质)。二氢丁苯那嗪位点占有率与去甲肾上腺素摄取抑制之间存在的相关性表明这些位点位于单胺转运体上。

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