Synthesis and in vitro evaluation of no-carrier-added 2-(3-(4-(4-[18F]fluorobenzyl)piperazin-1-yl)propyl)benzo[d]thiazole, a potential dopamine D4 receptor radioligand

被引：1

作者：

Li Gu-Cai ^{[1
]}

Zhang Ru ^{[1
]}

Xia Jiao-yun ^{[2
]}

机构：

[1] Hunan Inst Engn, Coll Chem & Chem Engn, Xiangtan 411104, Hunan, Peoples R China

[2] Changsha Univ Sci & Technol, Sch Chem & Biol Engn, Changsha Shi 410114, Hunan Sheng, Peoples R China

来源：

RADIOCHIMICA ACTA | 2016年 / 104卷 / 12期

关键词：

Fluorine-18; labeling; dopamine D4 receptor; benzo[d]thiazole; biological evaluation; ANTAGONISTS;

D O I：

10.1515/ract-2016-2597

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The dopamine D-4 receptor has been shown to play important roles in some central nervous system pathologies. Specific radioligands for the D-4 receptor may be useful to understand the function of the D-4 receptor and its correlations with various disorders. 2-(3-(4-(4-[F-18]Fluorobenzyl)piperazin-1-yl)propyl)benzo[d]thiazole ([F-18]4) was synthesized through a one-pot two-step procedure with total yield 18.6% (decay corrected). The specific activity of the radioligand was 112 GBq/mu mol and its radiochemical purity was >95.0%. Its affinity and selectivity for dopamine D-2-like receptors were measured through in vitro receptor binding evaluation and the K-i value for the D-4 receptor was determined to be 2.9 +/- 0.2 nM, and its selectivity for the dopamine D-4 receptor is 709-fold versus D-2long receptor, 823-fold versus D-3 receptor. The partition coefficient (Log D) of it was determined to be 2.6 +/- 0.1 through octanol-water partition experiment. The ligand presents desirable combination of lipophilicity, affinity and selectivity for the dopamine D-4 receptor. The results suggested that the radioligand shows promises for the in vivo study of the dopamine D-4 receptor.

引用

页码：897 / 903

页数：7

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