糖基化生长抑素的~(125)I标记及生物分布

Preparation and Biodistribution of ~(125)I Radiolabeled Glycosylated Somatostatin

  • 摘要: 以天然生长抑素、葡聚糖和酪胺为原料,合成了糖基化生长抑素(生长抑素-葡聚糖-酪胺);以125I-奥曲肽(125I-Tyr3-Octreotide)为放射配基,进行受体竞争结合实验,测定了糖基化生长抑素的IC50;并观察了125I标记的糖基化生长抑素在正常SD大鼠体内的分布和血液清除状况。结果表明:糖基化的生长抑素保持了对生长抑素2型受体的高亲和力;其IC50与Octreotide相近,125I标记的糖基化生长抑素血液半减期为6.7h,主要浓聚肝、脾脏并经肾排泄,肾上腺具有较高的放射性摄取,且24 h内基本保持不变,125I标记的糖基化生长抑素对生长抑素受体阳性组织具有靶向性。

     

    Abstract: Natural somatostatin,dextran-10 and tyramine are used to synthesis somatostatin-dextran-tyramine(SMS-Dx~(10)-tyramine,glycosylated somatostatin).The somatostatin receptor competition binding study of glycosylated somatostatin in vitro is carried out using rat brain cortex membranes(expressing somatostatin receptor type 2) and the radioligand of ~(125)I-Tyr~3-Octreotide.The radioiodinated glycosylated somatostatin is prepared by Iodogen method.The biodistribution and blood half life are investigated in normal rats.The glycosylated somatostatin posses high somatostatin type 2 receptor binding affinity,the same IC_(50)value as the reference ligand Octreotide,and the blood half-life is 6.7 h after post injection.The digestion and excretion is mainly through the hepatobiliary and kidney system.The adrenals gland has higher uptake,which is a somatostatin receptor positive organ.The radioiodinated glycosylated somatostatin shows promising properties and is worthy of further investigation.

     

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