This study describes the synthesis and radiosynthesis of eight new [¹⁸F]fluoro-inositol-based radiotracers in myo- and scyllo-inositol configuration. These radiotracers are equipped with a propyl linker bearing fluorine-18. This fluorinated arm is either on a hydroxyl group, i.e. O-alkylated inositols, or on the cyclohexyl backbone, i.e. C-branched derivatives. To modulate lipophilicity, inositols were synthesized in acetylated or hydroxylated form. Automated radiosynthesis was performed on the AllInOne module and the radiotracers were produced in good radiochemical yields (15–31.5% dc). Preliminary in vivo preclinical evaluation of these eight [¹⁸F]fluoro-inositols as Positron Emission Tomography (PET) imaging agents in a breast tumour-bearing mouse model was performed and compared with [¹⁸F]-2-fluoro-2-deoxy-d-glucose ([¹⁸F]FDG). Amongst the different inositols, [¹⁸F]myo-2 showed the highest tumour uptake 2.34 ± 0.39%ID/g, revealing the potential of this tracer for monitoring breast cancer.

这项研究描述了八种新的[ ¹⁸ F]氟肌醇基放射性示踪剂的合成和放射性合成，这些示踪剂是肌醇和鞘氨醇。这些放射性示踪剂配备了带有氟18的丙基接头。该氟化臂在羟基上，即在O-烷基化的肌醇上，或在环己基主链上，即在C-支链的衍生物上。为了调节亲脂性，以乙酰化或羟基化形式合成了肌醇。在AllInOne模块上进行了自动放射合成，并且放射性示踪剂的放射化学产率很高（直流15–31.5％）。初步体内这八个[的临床前评价¹⁸F]进行比较氟-肌醇作为正电子发射断层扫描（PET）中乳腺肿瘤轴承小鼠模型成像剂与[ ¹⁸ F] -2-氟-2-脱氧d -葡萄糖（[ ¹⁸ F] FDG） 。在不同的肌醇中，[ ¹⁸ F] myo -2显示最高的肿瘤吸收率2.34±0.39％ID / g，这表明该示踪剂具有监测乳腺癌的潜力。