Abstract:
Natural somatostatin (SMS), dextran-10(Dx
10) and cysteamine were used to synthesis somatostatin-dextran-cysteamine (SMS-Dx
10-Cysteamine) conjugate. The
in vitrosomatostatin receptor competition binding study was carried out by using
125I-Tyr
3-Octreotide as a radioligand to measure the IC
50value of SMS-Dx
10-Cysteamine. The SMS-Dx
10-Cysteamine was radiolabeled with
99Tc
m by using gluconate as a transchelator. The radiolabeling conditions of 99Tc
mCysteamine-Dx
10-SMS and its
in vitrostability were studied in detail. The biodistribution and blood halflife of
99Tc
m-Cysteamine-Dx
10-SMS were investigated in normal rats and its tumor uptake and imaging properties were evaluated in nude mice bearing human pancreatic tumor. The results show that SMS-Dx
10-Cysteamine remained high receptor binding affinity to somatostatin receptor subtype 2, and the IC
50value is in the same range as somatostatin. The radiolabeling efficiency of
99Tc
m-CysteamineDx
10-SMS is about 85% under optimum conditions and its radiochemical purity is more than 99% after purification. The blood halflife of
99Tc
m-Cysteamine-Dx
10-SMS in normal rats is 2.38 h post injection. The digestion and excretion is mainly through the hepatobiliary and kidney system. The
99Tc
m-Cysteamine-Dx
10-SMS is localized in pancreatic tumor and show visible tumor uptake at 6 h imaging. The results indicate that
99Tc
m-Cysteamine-Dx
10-SMS is a promising imaging agent candidate for somatostatin receptor positive tumor.