^(111)In-DTPA-D-Phe^1-octreotide的动物实验

Animal experiment of ^(111)In-DTPA-D-Phe^1-octreotide

Somatostatin受体阳性肿瘤显像剂111In－DTPA－D－Phe1－octreotide在体内降解产物为111In－DTPA，给药后3h血中111In－DTPA占血中放射性的50％，尿中为40％。正常鼠与载胰腺癌裸鼠的动物实验表明：该显像剂的血液清除很快，注射后10min血液的％ID／g为注射后1min的50％；放射性主要从泌尿系统排泄，给药后4min膀胱显影，至30min双肾和膀胱的放射性含量达50％ID；T／B比值在给药后逐渐增高，至24h可达7．92；给药后0．5－24h均可进行载胰腺癌裸鼠模型上的肿瘤阳性显像，24h时相的图像质量最佳。

The animal experiments of a novel somatostatin receptor-positive tumorsimaging agent, 111In- DTPA - D - Phe1 - octreotide, has been described. Biologicalproperties were evaluated by dynamic and static γ images of somatostatinreceptor-positive tumors in nude mice bearing pancreatic carcinoma. Theradiocomponent of 111In-DTPA, which came from 111In-DTPA-D-Phe1-octreotidedecomposition, showed 50% of radioactivity in blood and 40% in urine at 3hpostinjection. Rapid blood and urine clearance, and high T/B ratio (7.92 up to 24hpostinjection) were observed. The images of somatostatin receptor-positive tumorscould be obtained during 0.5- 24h after administration but the best one would be at24h.