A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.
A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.
复制标题
基于吡咯戊酮的多巴胺转运蛋白的新型光亲和配体。
DOI：
10.1016/j.bmc.2009.04.057
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发表时间：
2009
影响因子：
3.5
通讯作者：
Vaughan,RoxanneA
中科院分区：
文献类型：
--
作者：
Lapinsky,DavidJ;Aggarwal,Shaili;Huang,Yurong;Surratt,ChristopherK;Lever,JohnR;Foster,JamesD;Vaughan,RoxanneA
与基于托烷的化合物如可卡因相比，多巴胺转运蛋白（DAT）的非基于托烷的光亲和配体相对未被探索。为了填补这一知识空白，合成了一种配体，其中吡咯戊酮的芳环被光反应性叠氮基取代。类似物1-（4-叠氮基-3-碘苯基）-2-吡咯烷-1-基-戊-1-酮表现出对DAT的明显结合亲和力（Ki=78± 18 nM），表明放射性碘标记的形式在该蛋白的结构-功能研究中的潜在用途。
Non-tropane-based photoaffinity ligands for the dopamine transporter (DAT) are relatively unexplored in contrast to tropane-based compounds such as cocaine. In order to fill this knowledge gap, a ligand was synthesized in which the aromatic ring of pyrovalerone was substituted with a photoreactive azido group. The analog 1-(4-azido-3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one demonstrated appreciable binding affinity for the DAT (Ki=78±18nM), suggesting the potential utility of a radioiodinated version in structure-function studies of this protein.