Study on labelling methods of<sup>125</sup>I-RC-160 and its biodistribution in animals

WANG Jing  WANG Xiqing  WANG Liangang  LI Fujun  DENG Jinglan

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Study on labelling methods of¹²⁵I-RC-160 and its biodistribution in animals

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- Study on labelling methods of¹²⁵I-RC-160 and its biodistribution in animals
- NUCLEAR TECHNIQUES Issue 11, (2002)
- 作者机构：
  
  1. 第四军医大学西京医院核医学科
  2. 第四军医大学西京医院实验外科
  3. 第四军医大学西京医院核医学科,西安,710032
- 作者简介：
- 基金信息：
  
  国家自然科学基金资助项目 (395 0 0 0 35 ,39870 2 18);全军医药卫生科研基金资助课题 (0 1MB12 0 )
- DOI：
  CLC： R817.1
- Published：01 November 2002
- 稿件说明：
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[1]汪静,王喜青,王连刚,李富军,邓敬兰.~(125)I-RC-160的标记方法研究及其正常小鼠体内的分布特征[J].核技术,2002(11):897-900.

WANG Jing WANG Xiqing WANG Liangang LI Fujun DENG Jinglan. Study on labelling methods of¹²⁵I-RC-160 and its biodistribution in animals[J]. Nuclear techniques, 2002, (11): 897-900.
[1]汪静,王喜青,王连刚,李富军,邓敬兰.~(125)I-RC-160的标记方法研究及其正常小鼠体内的分布特征[J].核技术,2002(11):897-900. DOI：

WANG Jing WANG Xiqing WANG Liangang LI Fujun DENG Jinglan. Study on labelling methods of¹²⁵I-RC-160 and its biodistribution in animals[J]. Nuclear techniques, 2002, (11): 897-900. DOI：

摘要

研究了一种高效碘标多肽RC - 16 0的方法

在其中以溴代琥珀酰亚胺（NBS）为氧化剂

常规氯胺T法作为对照。对12 5I -RC - 16 0的标记率、比活度进行了评价

并观察12 5I -RC - 16 0在正常小鼠体内的生物分布特征。结果显示 :在丙酮:生理盐水 =1:1体系中

测得12 5I -RC - 16 0的标记率NBS法为 92 %

比活度为 1.95× 10 12 Bq/mmoL

标记率随NBS用量增加而增高

最佳用量比为RC - 16 0 （μg）:12 5I（MBq）:NBS（μg） =3:7.4:1

且产物无需纯化 ;Ch -T法标记率为5 6 %

比活度为 0 .6 5× 10 12 Bq/mmoL

经SepPaK -C18反向色谱柱纯化

12 5I -RC - 16 0的标记率可达 92 %。标记物在血中清除较快

注射后不到 1h血中的放射性就下降了 87.2 %;12 5I -RC -16 0在甲状腺及肾的浓集度很低

主要经过消化系统排出体外。

Abstract

A method for the iodination of peptide RC-160 with high efficiency was developed. RC-160 was iodinated with N-bromosuccinimide (NBS) as oxidant

the conventional chloramine T (Ch-T) method was used as control. The labelling condition of NBS method was optimized and radiolabelled conjugate 125I-RC-160 was assessed as follows: no further purification was needed

the measured labelling yield of 125I-RC-160 was 92% and the specific activity was 1.95×10 12Bq/mmoL. The yield increased as the amount of NBS increased. The optimal ratio of RC-160(μg): 125I(MBq):NBS(μg)was 3:7.4:1. For Ch-T method

the labelling yield is 56% and specific activity was 0.65×10 12Bq/mmoL

but after purification by SepPaK-C 18

the labelling yield may reach as high as 92%. 1h after injection

radioactivity in blood decreased by 87.2%. No obvious concentration of 125I-RC-160 in thyroid or kidney was observed.

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Study on labelling methods of125I-RC-160 and its biodistribution in animals

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摘要

Abstract

关键词

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Study on labelling methods of¹²⁵I-RC-160 and its biodistribution in animals