Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104, USA.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3482-5. doi: 10.1016/j.bmcl.2010.05.007.
Three new 18F labeled fluoroalkyl tyrosine derivatives, O-(2-[18F]fluoroethyl)-alpha-methyltyrosine (FEMT, [18F]2), O-(2-[18F]fluoroethyl)-2-L-azatyrosine (FEAT, [18F]3), O-(2-[18F]fluoroethyl)-L-tyrosineamide (FETA, [18F]4) have been synthesized and radiofluorinated with 5-34% decay-corrected yield. In vitro studies were carried out in U-138 MG human glioblastoma. Cellular uptake of new tracers was compared to clinically utilized imaging agent O-(2-[18F]fluoroethyl)-L-tyrosine (FET, [18F]1). The uptake of tracers followed the order of FET ([18F]1) > FEAT([18F]3) > FEMT ([18F]2) approximately FETA ([18F]4).
三种新型 18F 标记的氟烷基酪氨酸衍生物，O-(2-[18F] 氟乙基)-α-甲基酪氨酸（FEMT，[18F]2）、O-(2-[18F] 氟乙基)-2-L-氮杂酪氨酸（FEAT，[18F]3）、O-(2-[18F] 氟乙基)-L-酪氨酸酰胺（FETA，[18F]4）已被合成并通过放射性氟化以 5-34%的衰变校正产率进行标记。在 U-138 MG 人神经胶质瘤中进行了体外研究。新示踪剂的细胞摄取与临床使用的成像剂 O-(2-[18F] 氟乙基)-L-酪氨酸（FET，[18F]1）进行了比较。示踪剂的摄取顺序为 FET([18F]1) > FEAT([18F]3) > FEMT([18F]2) 约等于 FETA([18F]4)。
