In this study, we developed a saccharin (SAC)‐based radiopharmaceutical (⁶⁸Ga‐NOTA‐SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)‐overexpressed tumors. We did a water‐soluble tetrazolium assay and flow cytometry analysis to identify the cell viability decrease by SAC. The radiochemical purity and stability of ⁶⁸Ga‐ NOTA‐SAC in human and mouse serum was greater than 98%. The small animal PET image‐based radioactivity distribution of all organs decreased over time.⁶⁸Ga‐NOTA‐SAC presented the highest tumor‐to‐muscle ratio at 90 min post injection (p.i). The growth rates of tumor‐to‐muscle ratios of ⁶⁸Ga‐NOTA‐SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of ⁶⁸Ga‐NOTA‐SAC as a PET tracer is expected to contribute to the diagnostic research on CA IX‐overexpressed tumors with the advantages of a relatively simple synthesis method.

中文翻译：

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使用人工甜味剂糖精开发碳酸酐酶 IX 过表达肿瘤的 68Ga 标记 PET 示踪剂

在这项研究中，我们开发了一种基于糖精 (SAC) 的放射性药物 ( ⁶⁸ Ga-NOTA-SAC)，并评估了其作为 PET 示踪剂在诊断碳酸酐酶 IX (CA IX) 过表达肿瘤中的应用可能性。我们进行了水溶性四唑测定和流式细胞术分析，以确定 SAC 导致的细胞活力降低。⁶⁸ Ga-NOTA-SAC在人和小鼠血清中的放射化学纯度和稳定性均大于98%。所有器官的基于小动物 PET 图像的放射性分布随着时间的推移而下降。⁶⁸ Ga-NOTA-SAC 在注射后 90 分钟 (pi) 呈现出最高的肿瘤与肌肉比率。肿瘤与肌肉比率的增长率为⁶⁸Ga-NOTA-SAC 在 60 分钟时为 88%，在 90 分钟时为 220%，与 30 分钟 pi 相比⁶⁸ Ga-NOTA-SAC 作为 PET 示踪剂的潜力预计将有助于 CA IX 过表达肿瘤的诊断研究具有合成方法相对简单的优点。