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Radiosynthesis challenges of 11C and 18F-labeled radiotracers in the FX2C/N tracerlab and their validation through PET-MR imaging.
Applied Radiation and Isotopes ( IF 1.6 ) Pub Date : 2020-10-20 , DOI: 10.1016/j.apradiso.2020.109486
Raman Kumar Joshi 1 , Nerella Sridhar Goud 1 , Chandana Nagaraj 1 , Dinesh Kumar 1 , Gopinath R 1 , Naren P Rao 2 , Anmol Dhawan 3 , Ahana Bhattacharya 1 , Sandhya Mangalore 1 , Rose Dawn Bharath 1 , Pardeep Kumar 1
Affiliation  

Glucose is the renowned source of the energy for the cancer growth, that's the reason for [18F]FDG success and make it widely used radiotracer. Though [18F]FDG has its own inherent limitations therefore many tracers have been developed to target specific receptors, and other metabolic routes. We have used FX2C and FX2N Tracerlab modules for the synthesis of the [11C]methionine, [18F]choline and [18F]fluorodopa via nucleophilic pathway in FX2N module. [11C]methionine was standardized in FX2C module using two different precursors, purified using C18 cartridge based technique. [18F]methylcholine was synthesized using dimethylaminoethanol precursor and purified using cartridge-based method. [18F]fluorodopa was synthesized using nucleophilic precursor and purified using in-built preparative HPLC on FX2N module. All radioactive intermediates and chemical impurities were evaluated by analytical HPLC. The radiochemical purity of D and L-[11C]methionine were 4.6 ± 3.2% and 95.4 ± 3.6% with other chemical impurities were less than prescribed limits with yield of 20 ± 5%. [18F]fluoromethylcholine was prepared with high radiochemical yield of 97.3 ± 2.6% with yield of 8 ± 3%. [18F]fluorodopa was synthesized with high radiochemical yield of 95.8 ± 1.4% with 15 ± 3% yield. The adaptation of [18F]fluorodopa synthesis to FX2N module via designing synthesis sequence and purified through on-line HPLC has provided high radiochemical purity. PET-MR imaging was done using these tracers which have validated the synthesis and their availability for future clinical applications.



中文翻译:

FX2C/N 示踪实验室中 11C 和 18F 标记放射性示踪剂的放射合成挑战及其通过 PET-MR 成像的验证。

葡萄糖是著名的癌症生长能量来源,这就是 [ 18 F] FDG 成功并使其广泛使用的放射性示踪剂的原因。尽管[ 18 F]FDG 有其固有的局限性,因此已经开发了许多示踪剂来靶向特定受体和其他代谢途径。我们已使用 FX2C 和 FX2N Tracerlab 模块通过 FX2N 模块中的亲核途径合成 [ 11 C] 蛋氨酸、[ 18 F] 胆碱和 [ 18 F] 氟多巴。[ 11 C] 蛋氨酸在 FX2C 模块中使用两种不同的前体进行标准化,并使用基于 C18 柱的技术进行纯化。[ 18F] 甲基胆碱是使用二甲氨基乙醇前体合成的,并使用基于墨盒的方法进行纯化。[ 18 F] 氟多巴是使用亲核前体合成的,并使用内置的制备型 HPLC 在 FX2N 模块上进行纯化。所有放射性中间体和化学杂质均通过分析型 HPLC 进行评估。D和L-[ 11 C]蛋氨酸的放射化学纯度分别为4.6±3.2%和95.4±3.6%,其他化学杂质均低于规定限度,产率为20±5%。[ 18 F]氟甲基胆碱以97.3±2.6%的高放射化学产率制备,产率为8±3%。[ 18 F]氟多巴以95.8 ± 1.4%的高放射化学产率合成,产率为15 ± 3%。[ 18]的适应F]氟多巴通过设计合成序列合成为FX2N模块并通过在线HPLC纯化,提供了高放射化学纯度。PET-MR 成像是使用这些示踪剂完成的,这些示踪剂已经验证了合成及其在未来临床应用中的可用性。

更新日期:2020-10-30
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