Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3.
Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3.
复制标题
新型放射性标记高亲和力胆碱转运蛋白抑制剂[11C]hemicholinium-3和[18F]hemicholinium-3的合成和生物分布。
DOI：
10.1016/j.bmcl.2007.01.105
复制
发表时间：
2007
影响因子：
2.7
通讯作者：
DeGrado,TimothyR
中科院分区：
文献类型：
--
作者：
Zheng,Qi-Huang;Gao,Mingzhang;Mock,BruceH;Wang,Shuyan;Hara,Toshihiko;Nazih,Rachid;Miller,MichaelA;Receveur,TimJ;Lopshire,JohnC;Groh,WilliamJ;Zipes,DouglasP;Hutchins,GaryD;DeGrado,TimothyR
高亲和力胆碱转运蛋白（CHT 1）系统是开发正电子发射断层扫描（PET）生物标志物以探测脑、心脏和癌症疾病的有吸引力的靶点。通过使用阳离子交换CM Sep-Pak柱的固相萃取（SPE）技术，已经很好地开发了新的放射性标记的CHT 1抑制剂[11 C]hemicholinium-3和[18F]hemicholinium-3的有效且方便的合成。通过在9 L-胶质瘤大鼠中的生物分布研究对两种示踪剂进行了初步评价，观察到心脏和肿瘤中的摄取，而观察到非常低的脑摄取。
The high-affinity choline transporter (CHT1) system is an attractive target for the development of positron emission tomography (PET) biomarkers to probe brain, cardiac, and cancer diseases. An efficient and convenient synthesis of new radiolabeled CHT1 inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3 by solid-phase extraction (SPE) technique using a cation-exchange CM Sep-Pak cartridge has been well developed. The preliminary evaluation of both tracers through biodistribution studies in 9L-glioma rats has been performed, and the uptakes in the heart and tumor were observed, while very low brain uptake was seen.