Synthesis, Radiolabeling, and Biological Evaluation of the trans-Stereoisomers of 1-Amino-3-(fluoro-18F)-4-fluorocyclopentane-1-carboxylic Acid as PET Imaging Agents,ACS Pharmacology & Translational Science

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Synthesis, Radiolabeling, and Biological Evaluation of the trans-Stereoisomers of 1-Amino-3-(fluoro-18F)-4-fluorocyclopentane-1-carboxylic Acid as PET Imaging Agents
ACS Pharmacology & Translational Science ( IF 4.9 ) Pub Date : 2021-04-05 , DOI: 10.1021/acsptsci.1c00062
Thomas C Pickel _{1,

2} , Gouthami Pashikanti ₁ , Ronald J Voll _{3,

4} , Weiping Yu _{3,

4} , Zhaobin Zhang ₃ , Jonathon A Nye _{3,

4} , John Bacsa _{1,

2,

3,

4} , Jeffrey J Olson ₃ , Lanny S Liebeskind ₁ , Mark M Goodman _{3,

4}

Affiliation

The enantiomeric non-natural cyclic amino acids (3R,4R)-1-amino-3-fluoro-4-(fluoro-¹⁸F)cyclopentane-1-carboxylic acid and (3S,4S)-1-amino-3-fluoro-4-(fluoro-¹⁸F)cyclopentane-1-carboxylic acid ([¹⁸F]5) have been prepared as a racemic mixture in 1.3% decay corrected radiochemical yield and in greater than 99% radiochemical purity. [¹⁸F]5 is transported primarily via system L with some transport occurring via system ASC, as assessed in rat 9L gliosarcoma, human U87 ΔEGFR glioblastoma, and human DU145 androgen-independent prostate carcinoma tumor cells. In rats bearing intracranial 9L gliosarcoma, [¹⁸F]5 gave tumor to contralateral brain tissue ratios of up to 2.8. Biodistribution studies in healthy rats demonstrated that bladder accumulation is delayed until 10 min postinjection.

中文翻译：

作为 PET 成像剂的 1-Amino-3-(fluoro-18F)-4-fluorocyclopentane-1-carboxy 酸的反式立体异构体的合成、放射性标记和生物学评价

对映体非天然环状氨基酸 (3 R ,4 R )-1-amino-3-fluoro-4-(fluoro- ¹⁸ F)cyclopentane-1-carboxy 酸和 (3 S ,4 S )-1-amino -3-氟-4-(氟- ¹⁸ F)环戊烷-1-羧酸 ( [ ¹⁸ F]5 ) 已制备为外消旋混合物，具有 1.3% 的衰变校正放射化学产率和大于 99% 的放射化学纯度。[ ¹⁸楼]5如在大鼠 9L 胶质肉瘤、人 U87 ΔEGFR 胶质母细胞瘤和人 DU145 雄激素非依赖性前列腺癌肿瘤细胞中评估的，主要通过系统 L 转运，其中一些转运通过系统 ASC 发生。在患有颅内 9L 胶质肉瘤的大鼠中，[ ¹⁸ F]5使肿瘤与对侧脑组织的比率高达 2.8。健康大鼠的生物分布研究表明，膀胱蓄积延迟到注射后 10 分钟。

更新日期：2021-06-11

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