) and a bifunctional chelator 2- methyl-6-(p-amidobenzyl) -diethylenetriaminepentaacetic acid (1B4M-DTPA) were used to synthesize a novel somatostatin-dextran-DTPA (SMS-Dx
70
-DTPA) conjugate and radiolabeled with
90
Y. An in vitro somatostatin receptor competition binding study was carried out by using
125
I-Tyr
3
-Octreotide as a radioligand to measure the IC
50
value of SMS-Dx
70
-DTPA. Bio- distribution and blood half-life of
90
Y-DTPA-Dx
70
-SMS were investigated in normal rats. The results show that SMS-Dx70-DTPA has a high receptor binding affinity to somatostatin receptor subtype 2
with the IC
50
value being in the same range as somatostatin. The blood half-life of
90
Y-DTPA-Dx
70
-SMS in normal rats was 6.39h post-injection. Digestion and excretion of
90
Y-DTPA-Dx
70
-SMS was mainly through the hepatobiliary and kidney systems. Increased uptake was seen in the adrenals and pancreas
and it kept almost constant during 24h. Therefore
90
Y-DTPA-Dx
70
-SMS has targeting properties towards somatostatin receptor positive organs and it may become a promising therapeutic agent candidate for somatostatin receptor positive tumors.