Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.
复制标题
具有最佳亲脂性的潜在正电子发射断层扫描 (PET) 配体的设计、合成和结合亲和力，用于多巴胺 D3 受体的脑成像。
DOI：
10.1016/j.bmc.2008.11.044
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发表时间：
2009
影响因子：
3.5
通讯作者：
R. Perrone
中科院分区：
文献类型：
--
作者：
M. Leopoldo;E. Lacivita;Paola De Giorgio;M. Contino;F. Berardi;R. Perrone
在寻找有潜力作为正电子发射断层扫描放射性配体用于大脑 D3 受体成像的化合物时，合成了一系列具有适当亲脂性 (2<logP<3.5) 的 N-[4-(4-芳基哌嗪-1-基)丁基]芳基甲酰胺并进行了体外测试。一些最终化合物表现出中等到高的多巴胺 D3 受体亲和力，但缺乏对 D2 受体的选择性。
In the search for compounds with potential for development as positron emission tomography radioligands for brain D3receptor imaging, a series of N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides with appropriate lipophilicity (2<logP<3.5) were synthesized and tested in vitro. Some of the final compounds showed moderate-to-high dopamine D3receptor affinities but lacked selectivity over D2receptors.
影响因子：
3.1
作者：
Laruelle, Marc;Slifstein, Mark;Huang, Yiyun
通讯作者：
Huang, Yiyun