[18F]FDG-Labeled CGPRPPC Peptide Serving as a Small Thrombotic Lesions Probe, Including a Comparison with [99mTc]-Labeled Form.

ABSTRACT

Purpose: Fibrin is a perfect target for specific imaging of all types of thrombotic lesions. Cyclic peptides were introduced as the best scaffolds out of the different types of probes for thrombi detection. This study was conducted to label previously synthesized peptide-targeting fibrin with [18F]FDG and its in vitro and in vivo assessments. Materials and Methods: CGPRPPC peptide functionalized with 6-hydrazinonicotinamide and Eei-NHS was synthesized and cyclized using air oxidation method. The cyclic sequences were labeled with [18F]FDG at 85°C within 30 min. The stability studies were performed in human plasma. Fibrin-binding and platelet aggregation tests were performed in vitro. Biodistribution and scintigraphy imaging in normal mice and carotid thrombotic rat model were considered as in vivo studies. Results: Radiolabeled peptides show a good stability in human plasma and also high-affinity binding for human fibrin. Platelet aggregation test confirmed specific binding of radiopeptides to fibrin. A key problem with the authors' previous research was inability to detect small-vessel thrombi. The results of positron emission tomography/computed tomography scanning show high specific uptake of [18F]FDG-labeled CGPRPPC in small-sized thrombosis. Conclusion: The experiment revealed that radiolabeling of cyclic peptide (CGPRPPC) with [18F]FDG enables us to detect small thrombotic lesions in small animal models with high resolution.