Radiolabeled novel peptide for imaging somatostatin-receptor expressing tumor: synthesis and radiobiological evaluation

The aim of this study was to synthesis, a radiolabeled (99mTc) new somatostatin-analogue 6-hydrazinopyridine-3-carboxylic-acid (HYNIC)-Asn3-octreotate (99mTc-HYNIC-AATE), and to evaluate as a candidate for imaging somatostatin-receptor (SSTR)-positive tumors and also compare it with 99mTc-HYNIC-Tyr3-octreotide (99mTc-HYNIC-TOC). Synthesis was performed by Fmoc-solid-phase strategy and 99mTc labeled by SnCl2. Biodistribution and imaging properties of new radiopeptide were also studied in C6 tumor bearing rat. Radiolabeling was performed at high specific activities and it showed high binding-affinity for SSTR2. In biodistribution, radiopeptides have showed high and receptor-specific uptake in the SSTR2 positive organs, tumor with rapid renal excretion from non-target tissues. These results demonstrated that 99mTc-HYNIC-AATE is a new specific radioligand for scintigraphy of somatostatin-receptor-positive tumors.