The radioligand [¹⁸F]FPEB, used for PET imaging of the brain's metabotropic glutamate receptor subtype 5 (mGluR5), undergoes a thorough validation process to ensure its safety, efficacy, and quality for clinical use. The process starts by optimizing the synthesis of [¹⁸F]FPEB to achieve high radiochemical yield and purity. This study focuses on optimizing the radiolabeling process using an aryl-chloro precursor and validating the GMP production for clinical applications. Fully automated radiolabeling was achieved via one-step nucleophilic substitution reaction. [¹⁸F]FPEB was produced and isolated in high radioactivity and radiochemical purity. Throughout the validation process, thorough quality control measures are implemented. Radiopharmaceutical batch release criteria are established, including testing for physical appearance, filter integrity, pH, radiochemical purity, molar activity, radiochemical identity, chemical impurity, structural identity, stability, residual solvent, sterility, and endotoxin levels. In conclusion, the validation of [¹⁸F]FPEB involved a comprehensive process of synthesis optimization, quality control, which ensure the safety, efficacy, and quality of [¹⁸F]FPEB, enabling its reliable use in clinical PET. Here, we successfully radiolabeled and validated [¹⁸F]FPEB using aryl-chloro precursor according to GMP production for clinical application.

中文翻译：

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从芳基氯前体自动放射合成 mGluR5 PET 示踪剂 [18F]FPEB 并进行临床应用验证

用于大脑代谢型谷氨酸受体亚型 5 (mGluR5) PET 成像的放射性配体 [ ^{18 F]FPEB 经过彻底的验证过程，以确保其临床使用的安全性、有效性和质量。该工艺首先优化 [ 18} F]FPEB的合成，以实现高放射化学产率和纯度。本研究的重点是使用芳基氯前体优化放射性标记工艺并验证临床应用的 GMP 生产。通过一步亲核取代反应实现全自动放射性标记。 [ ¹⁸ F]FPEB 的生产和分离具有高放射性和放射化学纯度。在整个验证过程中，实施了彻底的质量控制措施。建立了放射性药物批次放行标准，包括物理外观、过滤器完整性、pH、放射化学纯度、摩尔活度、放射化学特性、化学杂质、结构特性、稳定性、残留溶剂、无菌和内毒素水平的测试。总之，[ ¹⁸ F]FPEB的验证涉及合成优化、质量控制的综合过程，确保了[ ¹⁸ F]FPEB的安全性、有效性和质量，使其能够在临床PET中可靠使用。在这里，我们根据临床应用的 GMP 生产，使用芳基氯前体成功地放射性标记和验证了 [ ^{18 F]FPEB。}