Several studies have suggested that neurotensin receptors (NTRs) and neurotensin (NT) greatly affect the growth and survival of pancreatic ductal adenocarcinoma (PDAC). Developing NTR-targeted PET probes could therefore be important for the management of a pancreatic cancer patient by providing key information on the NTR expression profile noninvasively. Despite the initial success on the synthesis of ¹⁸F-labeled NT PET probes, the labeling procedure generally requires lengthy steps including azeotropic drying of ¹⁸F. Using a straightforward chelation method, here we report the simple preparation of aluminum-¹⁸F-NOTA-NT starting from aqueous ¹⁸F. The cell binding test demonstrated that [¹⁹F]AlF-NOTA-NT maintained high receptor-binding affinity to NTR1. This probe was then further evaluated in NTR1 positive pancreatic tumor models (AsPC-1 and PANC-1). After the administration of [¹⁸F]AlF-NOTA-NT, small animal PET studies showed a high contrast between tumor and background in both models at 1 and 4 h time points. A blocking experiment was performed to demonstrate the receptor specificity: the tumor uptake in AsPC1 without and with blocking agent was 1.0 ± 0.2 and 0.1 ± 0.0%ID/g, respectively, at 4 h post injection. In summary, a NTR specific PET agent, [¹⁸F]AlF-NOTA-NT, was prepared through the simple chelation method. This NTR-targeted PET probe may not only be used to detect NTR1 positive pancreatic tumors (diagnosis), but also it may be fully integrated to NTR target therapy leading to personalized medicine (theranostic).

中文翻译：

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[ ¹⁸ F] AlF-NOTA-NT作为神经降压素受体1阳性胰腺癌PET药物的开发

多项研究表明，神经降压素受体（NTRs）和神经降压素（NT）会极大地影响胰腺导管腺癌（PDAC）的生长和存活。因此，开发NTR靶向PET探针通过无创地提供有关NTR表达谱的关键信息，对于胰腺癌患者的治疗可能非常重要。尽管在¹⁸ F标记的NT PET探针的合成方面取得了初步成功，但标记程序通常仍需要漫长的步骤，包括¹⁸ F的共沸干燥。使用简单的螯合方法，我们在此报告了铝¹⁸ F-NOTA-的简单制备方法。NT从¹⁸ F水溶液开始。细胞结合试验表明[ ¹⁹F] AlF-NOTA-NT维持对NTR1的高受体结合亲和力。然后在NTR1阳性胰腺肿瘤模型（AsPC-1和PANC-1）中进一步评估该探针。给予[ ¹⁸ F] AlF-NOTA-NT后，小型动物PET研究显示，在两个模型中，在1和4小时的时间点，肿瘤和背景之间的对比度很高。进行阻断实验以证明受体特异性：在注射后4 h，不含和含阻断剂的AsPC1中的肿瘤摄取分别为1.0±0.2％和0.1±0.0％ID / g。总之，一种NTR专用PET剂[ ¹⁸F] AlF-NOTA-NT，是通过简单的螯合方法制备的。这种靶向NTR的PET探针不仅可以用于检测NTR1阳性的胰腺肿瘤（诊断），而且可以完全整合到NTR靶标治疗中，从而产生个性化的药物（热疗）。