Synthesis and Preliminary Biological Evaluation of 68Ga-labeled GIPR Targeting Probe
Glucose-dependent insulinotropic polypeptide receptor(GIPR)is one of the important targets of neuroendocrine tumors(NETs).In this study,a novel GIPR targeting probe 68Ga-DOTA-GIP(1-30)-F-02 was constructed through the module for automatic labeling.The labeling yield,radiochemical purity,and in vitro stability of this probe were investigated.The biodistribution in normal ICR mice and Micro-PET/CT imaging of PC12-hGIP tumor-bearing mouse models were studied.The results showed that the automatic method for 68Ga-DOTA-GIP(1-30)-F-02 preparation was simple and convenient with a good radiochemical yield of(65.32±1.57)%,high radiochemical purity(>99%),and good in vitro stability.The results of biodistribution showed low uptakes of 68Ga-DOTA-GIP(1-30)-F-02 in normal tissues,mainly excreted through the renal urinary system.Micro-PET/CT imaging showed the uptake at the tumor site reached(6.51±1.03)%ID/g at 60 min post-injection which indicates good tumor imaging potentiality.The feasibility and specificity of the probe for GIPR-targeted imaging of neuroendocrine tumors were preliminarily demonstrated.
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