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3rd International Congress 3rd International of Nuclear Congress Medicine of Nuclear & 15th Medicine Iranian Annual & 15th Iranian Congress Annual of<br />

Nuclear Congress Medicine of Nuclear Medicine<br />

Shahid Beheshti Shahid Beheshti University University of Medical Sciences of Medical 19-21 Sciences May 201119-21 May 2011<br />

A new bombesin kit labeled with 99mTc for breast cancer<br />

imaging<br />

Mostafa Erfani (Gandomkar), Seyed Pejman Shirmardi<br />

Nuclear Science Research School<br />

Introduction: Tumors such as prostate, small cell lung<br />

cancer,breast, gastric and colon cancer are known to over express<br />

receptors to bombesin (BBN). In this study, a new bombesin<br />

analogue was labeled with 99mTc via HYNIC and tricine/EDDA as<br />

coligands and investigated further.<br />

Methods: HYNIC-GABA-Bombesin (7-14) NH2 was synthesized using<br />

a standard Fmoc strategy. Labeling with 99mTc was performed at<br />

100 C for 10 min and radiochemical analysis involved ITLC and HPLC<br />

methods. The stability of radiopeptide was checked in the presence of<br />

humane serum at 37C up to 24 h. The receptor bound internalization<br />

and externalization rates were studied in GRP receptor expressing<br />

PC-3 cells. Biodistribution of radiopeptide was studied in mice.<br />

Results: Labeling yield of 98% was obtained corresponding to a<br />

specific activity of 2.6 MBq/nmol. Peptide conjugate showed good<br />

stability in the presence of human serum. The radioligand showed<br />

high and specific internalization into PC-3 cells (14.63±0.41% at 4<br />

h). In biodistribution studies, a receptor-specific uptake was observed<br />

in GRP-receptor-positive organs so that after 4 h the uptakes in<br />

mouse pancreas was 1.2±0.13% ID/g.<br />

Conclusion: The prepared conjugate showed high accumulation in<br />

pancreas as a positive GRP receptor targeted tissue followed by<br />

excretion via the kidney. These promising characteristics make our<br />

new designed labeled peptide conjugate as a very suitable candidate<br />

for diagnostic of malignant tumors.<br />

Keywords: Radiolabeling, Bombesin, 99mTc, Tumor<br />

166

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