Synthesis, radioiodination and in vivo screening of novel potent iodinated and fluorinated radiotracers as melanoma imaging and therapeutic probes
Synthesis, radioiodination and in vivo screening of novel potent iodinated and fluorinated radiotracers as melanoma imaging and therapeutic probes
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DOI：
10.1016/j.ejmech.2012.11.047
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发表时间：
2013-05-01
影响因子：
6.7
通讯作者：
Chezal, Jean-Michel
中科院分区：
文献类型：
--
作者：
Maisonial, Aurelie;Billaud, Emilie M. F.;Chezal, Jean-Michel
为了开发用于单光子发射计算机断层扫描 (SPECT)/正电子发射断层扫描 (PET) 成像和黑色素瘤靶向放射性核素治疗的新型碘化和氟化配对放射性示踪剂，我们从之前描述的先导结构 3 开始，成功合成并用碘 125 七种新衍生物进行放射性标记。评估了这些放射性示踪剂与啮齿类动物黑色素瘤伽马闪烁显像成像的相关性。即使在早期时间点，肿瘤放射性摄取通常也很高且具有特异性（[I-125]39-42，注射后 3 小时为 12.1-18.3% ID/g），并且观察到从非靶器官的快速清除。此外，当使用相应的[I-131]标记类似物时，计算出的可递送至肿瘤的有效剂量通常高于注射的100 cGy/MBq（[I-131]39-42为98.9-150.5 cGy/MBq）。这些结果使得化合物39-42适合用于(i)用氟18标记后的黑色素瘤的PET成像和(ii)用碘131标记后的播散性黑色素瘤的靶向放射性核素治疗。 (C) 2013 Elsevier Masson SAS。版权所有。
In order to develop new iodinated and fluorinated matched-pair radiotracers for Single-Photon Emission Computed Tomography (SPECT)/Positron Emission Tomography (PET) imaging and targeted radionuclide therapy of melanoma, we successfully synthesized and radiolabelled with iodine-125 seven new derivatives, starting from our previously described lead structure 3. The relevance of these radiotracers for gamma scintigraphic imaging of melanoma in rodent was assessed. The tumoural radioactivity uptake was most often high and specific even at early time points (12.1-18.3% ID/g at 3 h p.i. for [I-125]39-42) and a fast clearance from the non-target organs was observed. Also, calculated effective doses that could be delivered to tumours when using corresponding [I-131]-labelled analogues were generally higher than 100 cGy/MBq injected (98.9-150.5 cGy/MBq for [I-131]39-42). These results make compounds 39-42 suitable candidates for (i) PET imaging of melanoma after labelling with fluorine-18 and (ii) targeted radionuclide therapy of disseminated melanoma after labelling with iodine-131. (C) 2013 Elsevier Masson SAS. All rights reserved.