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99m tcn nuclear mark compound, its preparation and application

A technology of 99mtcn and complexes, applied in the field of 99mTcN nuclear labeling complexes and their imaging agents in human and animal organs or tissues, to achieve clear imaging effects

Inactive Publication Date: 2005-02-23
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In the study of tumor radiopharmaceuticals, an interesting phenomenon has been discovered in recent years: the drug originally designed for myocardial perfusion imaging 201 Tl, 99m Tc-MIBI, 99m Tc-tetrofosmin and 99m Tc-furifosmin, however, can be used as a sensitive tool to detect tumor-specific molecular biological processes. Many studies on tumor cell experiments in vitro and tumor imaging experiments in vivo have been reported.

Method used

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  • 99m tcn nuclear mark compound, its preparation and application
  • 99m tcn nuclear mark compound, its preparation and application
  • 99m tcn nuclear mark compound, its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

example 1-3

[0037] Examples 1-3 are for preparing kits A to D, and the raw materials used, their dosages and pH conditions are shown in Table 2.

[0038] pill box

Pill box A

Pill box B

raw material

SDH

PDTA

SnCl 2 2H 2 o

pH

PNP1

Mannitol

pH

Example 1

1mg

1mg

0.2mg

7.0

0.2mg

50mg

7.0

Example 2

20mg

10mg

0.4mg

5.0

10mg

10mg

4.0

Example 3

5mg

5mg

0.05mg

7.5

2mg

10mg

5.0

[0039] pill box

Pill box C

Pill box D

raw material

DTC-like ligands

Mannitol

Na 2 HPO 4 ·

12H 2 o

pH

twain

-80

Anhydrous

ethanol

NOEt

DEDC

DBODC

Example 1

0.2mg

20mg

1mg

9.0

40mg

0.2mL

Example 2

10mg

40mg

40mg

5.0

400mg

0.2mL

Example 3

2mg

10mg

5mg

8.0

200mg

...

example 4

[0045] This example is [ 99m TcN(PNP1)(DTC)] + Preparation of (T) complexes

[0046] Take a volume of 2mL 99m TCO 4 - Fresh eluent (3.7-3700MBq) was injected into the kit A of Example 1-3, shaken evenly, and after the solid was completely dissolved, it was allowed to stand at room temperature for 15 minutes. Add the above solutions to the kit B of Example 1-3 respectively, shake well, take out the solutions respectively and add them to the kit C of Example 1-3, shake well, the solid dissolves completely quickly, heat to 80-100 ℃, maintain 15min. After cooling, take 0.1 mL of the solution in kit D of Examples 1-3 and add it to kit C, and shake well. Through TLC (thin layer chromatography) analysis, three kinds of [ 99m TcN(PNP1)(DTC)] + The radiochemical purity of (T) type complexes is greater than 95%.

example 5

[0048] This example is the [ 99m TcN(PNP1)(DBODC)] + Complex

[0049] Take a volume of 2mL 99m TCO 4 - Fresh eluent (3.7-3700MBq) was injected into the kit A of Example 3, shaken well, and after the solid was completely dissolved, it was allowed to stand at room temperature for 15 minutes. Add the above solution into kit B of Example 3, shake well, take out the solution and then add it to kit C of Example 3, shake well, the solid dissolves quickly and completely, heat to 80-100°C, and keep for 15 minutes. According to TLC analysis, the radiochemical purity of the complex is greater than 95%.

[0050] The following is an example of biological performance measurement

[0051] determination [ 99m TcN(PNP1)(DTC)] + (T) The biological performance of class complex, and do not add Tween-80 adjuvant with example 5 [ 99m TcN(PNP1)(DBODC)] + and widely used as myocardial perfusion imaging agents in the prior art 99m Tc-MIBI for comparison.

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PUM

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Abstract

A kind 99mTcN nuclear label coordinate compounds. Its general formula is [99mTcN (PNP1) (DTC) ]+ (T),, that 99mTcN stand for technetium nitrogen centre nucleon, PNP1 stand for diphosphineamine compounds, DTC stand for a amino sulfonate compounds,T as for Tween .- 80. The process is making drug box first, further prepares coordinate compounds needed with radiochemical purity greater than 95%. The prepared label coordinate compound by changing DTC coordinate group and adding auxiliary materials has higher cardiac muscle ingests, well retentivity, higher ratio of heart / liver, heart / lung etc. target / none-target. It can be used as developer for cardiac muscle perfusion or tumour in organs or tissues of human and animals.

Description

technical field [0001] The present invention relates to 99m TcN nuclear labeling complex and its application in human and animal organ or tissue imaging agents, especially in myocardial perfusion imaging agents and tumor imaging agents. Background technique [0002] Cardiovascular disease is one of the main diseases that seriously endanger people's health and life safety. Early diagnosis of cardiovascular disease is of great significance to the prevention and treatment of diseases. Cardiology uses myocardial radiopharmaceuticals for myocardial imaging, which can realize the early diagnosis of cardiovascular diseases, and plays an important role in the diagnosis of clinical myocardial ischemia, myocardial infarction and other diseases. Exercise or drug stress myocardial perfusion imaging using radionuclide markers is a mature technique for diagnosing and evaluating the degree of coronary artery disease. affim. [0003] For myocardial perfusion imaging agents, the amount of...

Claims

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Application Information

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IPC IPC(8): A61K51/00C07F13/00
Inventor 王学斌楚进锋唐志刚陆洁张俊波张现忠
Owner BEIJING NORMAL UNIVERSITY
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