Three amino acids residues of Arg-Gly-Asp (RGD) are often the primary site of recognition by integrins which are responsible for tumor invasion and metastasis. In this research
one peptides containing RGD: HCRGD(D)FC were radiolabeled with 188 Re-tricarbonyl complex. High radiolabeling ratios (>90%) were achieved under the reaction condition of 75℃
30min. The radiolabeled peptide got high stability in PBS at room temperature for 4 hours. The hemolysis of red blood cells was not observed during incubation at 37℃ for 3 hours. Biodistribution studies were performed in normal male mice and S180-bearing mice
respectively. The radioactivities were rapidly eliminated by the hepatobiliary and urinary systems. Tumor/Muscle ratios were 4.4075±0.1139
5.1510±0.5375
4.4727±0.4895 and 4.8788±3.16 at 1h
4h
24h and 48h after injection. The results showed that 188Re-tricarbonyl peptide containing RGD was a potential agent for tumor treatment.