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Glucose derivative complex marked with 99mTc, 188 Re or 186Re and its preparation process

A glucose derivative, 99mtc technology, applied in the field of glucose derivative complexes, can solve the problems of low equipment penetration rate, high cost of FDG, short half-life, etc.

Inactive Publication Date: 2012-09-05
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] because 18 FDG is expensive, requires medical cyclotron and PET imaging equipment, and the equipment penetration rate is not high (more than 60 units in the country), and the half-life is short ( 18 F half-life is 108min), difficult to popularize, and 99m Tc is cheap, convenient and easy to obtain, and the half-life and energy are suitable (T 1 / 2 =6.0h; γ: 150keV), and the penetration rate of imaging equipment SPECT is relatively high (500 units nationwide), so it needs to be developed clinically in recent years 99m Tc-labeled glucose analog

Method used

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  • Glucose derivative complex marked with 99mTc, 188 Re or 186Re and its preparation process
  • Glucose derivative complex marked with 99mTc, 188 Re or 186Re and its preparation process
  • Glucose derivative complex marked with 99mTc, 188 Re or 186Re and its preparation process

Examples

Experimental program
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Effect test

Embodiment 11

[0107] Example 1.1: [ 99m TcO] 3+ Nuclear labeling compound 1

[0108] Add 0.5mL water and 0.5mL ethanol to 2mg compound 1 to make a solution, add 0.3mL (10mCi / ml) freshly rinsed Na 99m TCO 4 , quickly add 0.2mlSnCl 2 Solution (1mg / mL, 0.1NHCl), adjust pH=8.0~8.5, react at room temperature for 20min, filter with 0.2μm filter membrane, monitor by TLC (acetonitrile / polyamide; normal saline / silica gel), calculate the labeling rate, the labeling rate is 99.26 %, HPLC monitoring (HPLC condition: A phase 0.1% trifluoroacetic acid aqueous solution; B phase 0.1% trifluoroacetic acid acetonitrile solution; Gradient: 0~10min: A=100%, B=0; 10~20min: A=50 %, B=50%; 20-30min: A=0, B=100%). HPLC retention time is 17.20min, 99.94%.

Embodiment 12

[0109] Example 1.2: [ 99m TcO] 3+ Nuclear labeling compound 3

[0110] Add 0.5mL water and 0.5mL ethanol to 2mg compound 3 to make a solution, add 0.3mL (10mCi / mL) freshly rinsed Na 99m TCO 4 , quickly add 0.2mlSnCl 2 Solution (1mg / mL, 0.1NHCl), adjust pH=8.0~8.5, react at room temperature for 20min, filter with 0.2μm filter membrane, monitor by TLC (acetonitrile / polyamide; normal saline / silica gel), calculate the labeling rate, the labeling rate is greater than 99%. HPLC monitoring (HPLC conditions: A phase 0.1% trifluoroacetic acid aqueous solution; B phase 0.1% trifluoroacetic acid acetonitrile solution; Gradient: 0~10min: A=100%, B=0; 10~20min: A=50%, B=50%; 20-30min: A=0, B=100%). HPLC retention time is 16.60min, 99.93%.

Embodiment 13

[0112] [ 99m TcO] 3+ Nuclear labeling compound 6

[0113] Add 0.5mL water and 0.5mL ethanol to 2~3mg compound 6 to make a solution, add 0.3mL (10mCi / mL) freshly rinsed Na 99m TCO 4 , quickly add 0.2mlSnCl 2 Solution (1mg / mL, 0.1NHCl), adjust pH=8.0~8.5, react at room temperature for 20min, filter with 0.2μm filter membrane, monitor by TLC (acetonitrile / polyamide; normal saline / silica gel), calculate the labeling rate, the labeling rate is greater than 99%. HPLC monitoring (HPLC conditions: A phase 0.1% trifluoroacetic acid aqueous solution; B phase 0.1% trifluoroacetic acid acetonitrile solution; Gradient: 0~10min: A=100%, B=0; 10~20min: A=50%, B=50%; 20-30min: A=0, B=100%). HPLC retention time is 16.70min, 86.00%; 18.20min, 13.88%.

[0114] [ 99m TcO] 3+ Nuclear labeling compound 2

[0115]Add 0.5mL water and 0.5mL ethanol to 2mg compound 2 to make a solution, add 0.3mL (10mCi / ml) freshly rinsed Na 99m TCO 4 , quickly add 0.2mlSnCl 2 Solution (1mg / mL, 0.1NHCl), a...

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Abstract

The present invention relates to glucose derivative complex marked with 99mTc, 188Re or 186Re and its preparation process. The glucose derivative complex has nuclear intermediate of [99mTcO]3+, [188 / 186ReO]3+, [99mTcN]2+, [188 / 186ReN]2+, [99mTc(CO)3(H2O)3]1+ or [188 / 186Re(CO)3(H2O)3]1+, and ligand with the general expression as shown. The glucose derivative complex marked with 99mTc, 188Re or 186Re has low cost, easy preparation, proper half life and energy, SPECT developing and wide application. R=methyl-ethyl-propyl-isopropyl-butyl-isobutyl.

Description

technical field [0001] The present invention relates to a 99m Tc, 188 Re or 186 Re-labeled glucose derivative complex and its preparation method. Background technique [0002] 18 F-FDG imaging principle: [0003] FDG is an analogue of glucose and is metabolized into FDG-6-phosphate after entering the cell. However, unlike glucose-6-phosphate, the former cannot be further metabolized and remains in the cell. Therefore, the metabolic rate of glucose can be obtained from the FDG retained in the tissue. [0004] Tumor imaging: Tumor cells and normal tissue cells have different glucose metabolism mechanisms. In tumor cells, due to the increased expression of glucose transport mRNA, the levels of glucose transporters Glut1 and Glut3, the level of hexokinase, and the glucose-6- The effect of multiple factors such as down-regulation of phosphatase levels makes 18 FDG, like glucose, has increased uptake in tumor cells. Therefore, PET can be used to accurately display the loca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
Inventor 朱霖刘锰刘亚静余媛
Owner BEIJING NORMAL UNIVERSITY
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