99Tcm-MAG3-K237的制备及其在健康动物体内的药代动力学和分布研究

杨明福; 刘广元; 李前伟

您当前的位置：

首页 >

文章列表页 >

⁹⁹Tc^m-MAG₃-K237的制备及其在健康动物体内的药代动力学和分布研究

论著 | 更新时间：2026-01-09

- ⁹⁹Tc^m-MAG₃-K237的制备及其在健康动物体内的药代动力学和分布研究
- Preparation of ⁹⁹Tc^m-MAG₃-K237 and its pharmacokinetics and distribution in health animals
- 陆军军医大学学报 2010年32卷第5期页码：482-485
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：
  中图分类号： {R914.2};R817.1;R969.1
- 纸质出版：2010
- 稿件说明：
移动端阅览
杨明福,刘广元,李前伟.99Tcm-MAG3-K237的制备及其在健康动物体内的药代动力学和分布研究[J].陆军军医大学学报(原第三军医大学学报),2010,32(05):482-485.

　Yang Mingfu,Liu Guangyuan,Li Qianwei.Preparation of 99Tcm-MAG3-K237 and its pharmacokinetics and distribution in health animals[J].J Amry Med Univ (J Third Mil Med Univ),2010,32(05):482-485.
杨明福,刘广元,李前伟.99Tcm-MAG3-K237的制备及其在健康动物体内的药代动力学和分布研究[J].陆军军医大学学报(原第三军医大学学报),2010,32(05):482-485. DOI：

　Yang Mingfu,Liu Guangyuan,Li Qianwei.Preparation of 99Tcm-MAG3-K237 and its pharmacokinetics and distribution in health animals[J].J Amry Med Univ (J Third Mil Med Univ),2010,32(05):482-485. DOI：

摘要

目的探讨

标记血管内皮生长因子受体2（vascular endothelial growth factor receptor-2，VEGFR-2，KDR）小分子拮抗肽K237的方法，研究标记物在健康动物体内的药代动力学特性及体内分布特点。方法化学方法合成制备MAG

-K237，并用

标记；鉴定标记物的理化性质；测定标记物经新西兰大白兔静脉注射后不同时相血液放射性浓度，得出最佳房室模型与药代动力学参数；分别测定经尾静脉注射7.4 MBq标记物后的昆明小鼠各器官质量和放射性计数，经参考源校正后计算各脏器每克组织百分注射剂量率（%ID/ｇ）；经耳缘静脉注射37 MBq标记物，在SPECT下观察其在兔体内的动态分布。结果

-MAG

-K237的放化纯度为（97.98±0.76）％，比活度为（3.54±0.03） TBq/mmol；室温（25 ℃）下保存8 h后放化纯度为（96.15±0.37）%；半胱氨酸置换率为0.2%～0.37%；不与血清蛋白结合；兔体内动力学过程符合权重为1/c

的三室模型，快分布相半衰期（t

1/2α

）、慢分布相半衰期（t

1/2β

）及消除相半衰期（t

1/2γ

）分别为（4.00±3.53）、（24.48±9.84）、（852.24±444.00） min，清除率（CL）为（1.833±0.408） ml/min；标记物在健康小鼠体内清除迅速，肾脏、肝脏及肠道分布较多，但肝脏30 min后分布很少。结论本研究制备的

-MAG

-K237的放射化学纯度高，体内外稳定性好，血液清除速度快，通过肾脏和肝脏双重途径代谢。

Abstract

Objective To explore how to label small molecule inhibitor K237 (HTMYYHHYQHHL) of vascular endothelial growth factor receptor-2

(VEGFR-2

KDR) with technetium 99m and to study pharmacokinetic characteristics and body distribution of the labeled peptide in healthy animals. Methods MAG3-K237 was prepared through chemosynthesis

and then labeled it with

. Then its stability and physicochemical properties were determined by paper chromatography. The best compartment model and its pharmacokinetic parameters were obtained through determining blood radioactive concentrations at 1.5

120

240 and 480 min after injection of 37 MBq

-MAG

-K237 into 6 rabbits. SPECT imaging was applied to investigate the dynamic distribution of the peptide in rabbits. After 7.4 MBq

-MAG

-K237 injected into 35 healthy mice via caudal vein

the mice were sacrificed in 1

120 and 240 min respectively after the injection (n=5 at each time point)

and then their samples of blood

heart

lungs

liver

spleen

intestine

muscle

bone and brain were collected to measure the weight and radioactive counting of each organ after injection

and to calculate %ID/g of each organ. Results The radiochemical purity of

-MAG

-K237 was (97.98±0.76)%

which was (96.15±0.37)% after 8 h being conserved under room temperature (25℃) and the cysteine replacement rate was from 0.2% to 0.37% and the labeled peptide could not combine with blood serum protein. Its dynamics in rabbits conformed to the three-compartment model with the weight of 1/c

and the main parameter were as follows: t

1/2α

1/2β

and t

1/2γ

were 4.00±3.53

24.48±9.84 and 852.24±444.00 min respectively; CL was 1.833±0.408 ml/min. SPECT imaging and distribution test in mice showed that the peptide could be quickly cleared from blood in healthy animals and distributed more in the kidney

liver and intestine

but its distribution in the liver became fewer in 30 min after injection. Conclusion We obtaine

d the

labeled peptide with high radiochemical purity (95%) and perfect stability

which could be quickly cleared from blood and excreted though liver and kidney.

关键词

Keywords

references

浏览量

下载量

CSCD

文章被引用时，请邮件提醒。

提交

工具集

关联资源

柚皮苷改善脂多糖诱导的小鼠抑郁样行为的作用研究

组织蛋白酶K在酒精性心肌病小鼠心功能不全中的作用及其损伤机制研究

柴胡口服液改善成年BTBR自闭症小鼠海马神经发生及短期记忆缺陷

α-酮戊二酸对小鼠胆汁淤积性肝损伤的缓解作用

CX3CR1沉默介导的巨噬细胞极化减轻CCl4诱导的小鼠肝纤维化