生长抑素受体拮抗剂^(68)Ga-NODAGA-JR11的制备及初步生物学评价

The Preparation and Preliminary Biological Evaluation of Somatostatin Receptor Antagonist ^(68)Ga- NODAGA- JR11

目的 制备特异性生长抑素受体拮抗剂^(68)Ga-NODAGA-JR11,探讨其用于神经内分泌肿瘤PET显像的可行性。方法本研究合成了生长抑素受体拮抗剂NODAGA-JR11,并采用比利时IRE公司药用级^(68)Ge/^(68)Ga发生器获得高比活度的^(68)GaCl_(3)溶液进行了^(68)Ga-NODAGA-JR11的制备。结果 经过多次的放射性标记实验(n≥15),得到的标记物^(68)Ga-NODAGA-JR11放化纯均可以保持在95%以上,制备工艺稳定可靠、重现性高。结论^(68)Ga-NODAGA-JR11具有良好的水溶性和良好的体外稳定性,在荷AR42J肿瘤鼠的micro-PET/CT显像中显示了良好的SSTR靶向性和特异性。68Ga标记的NODAGA-JR11冻干药盒的初步研究及标记表明,所制备的NODAGA-JR11冻干药盒可用于^(68)Ga的标记。

Objective To conduct preparation of specific SSTR probes ^(68)Ga-NODAGA-JR11 and evaluate its feasibility for PET imaging in NETs.Methods In the current study,the somatostatin receptor antagonist NODAGA-JR11 was synthesized,and 68 Ga-NODAGA-JR11 was prepared using ^(68)GaCl_(3) solution obtained with IRE medical grade ^(68)Ge/^(68)Ga generator.Results The radiochemical purity of products was maintained above 95%after more than 15 experiments,and the preparation process was stable and reliable with high reproducibility.Conclusion ^(68)Ga-NODAGA-JR11 shows an excellent water solubility and in vitro stability as well as a good SSTR targeting and specificity in micro-PET/CT imaging in tumor-bearing mice for this radiopharmaceutical.The preliminary study of the NODAGA-JR11 freeze-dried kits for ^(68)Ga labeling and the validation of the ^(68)Ga labeling results show that the prepared NODAGA-JR11 freeze-dried kits can be used for ^(68)Ga labeling.