Technetium-99m marked dimercapto propionamido novel lactose albumin complexes, preparation and use thereof

A technology based on dimercaptopropionamide and albumin, which is applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of destroying protein structure, low Tc binding ability, affecting biological performance, etc., and achieves simple preparation, initial uptake value and target The effect of high chemical purity and low cost of use

Inactive Publication Date: 2009-07-22
BEIJING NORMAL UNIVERSITY +1
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Problems solved by technology

but 99m Tc-GSA still exists 99m Disadvantages such as low Tc binding ability and slightly higher kidney uptake
In 2004, Jeong et al. used β-mercaptoethanol to reduce LSA (neolactosyl human serum albumin) to obtain ligands containing sulfhydryl groups. 99m After Tc labeling, it shows good stability and excellent biological performance, but the structure of the protein will be destroyed by reducing the disulfide bond, which will affect its biological performance in vivo

Method used

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  • Technetium-99m marked dimercapto propionamido novel lactose albumin complexes, preparation and use thereof
  • Technetium-99m marked dimercapto propionamido novel lactose albumin complexes, preparation and use thereof
  • Technetium-99m marked dimercapto propionamido novel lactose albumin complexes, preparation and use thereof

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Embodiment Construction

[0037] The present invention is described in detail below through examples, a technetium-99m-labeled 6-hydrazinopyridine-3-carboxamide-based neolactoalbumin complex:

[0038] (1) Preparation of DMP-NGA

[0039] Take 0.86g of 2,3-diacetylthiopropionic acid dicyclohexylamine salt into a small beaker, add 4mL of ethyl acetate, stir to obtain a white suspension, slowly add 10% hydrogen sulfate dropwise under stirring Potassium solution, acidify until the solution is clear, and extract with 40mL×3 ethyl acetate. The resulting pale yellow organic phase was dried over anhydrous sodium sulfate overnight. After suction filtration, the solvent was removed by rotary evaporation to obtain 0.48 g of white solid. Yield 93.8%.

[0040] In a 25 mL three-necked flask, the obtained white solid was dissolved in 4 mL of dichloromethane, cooled to 0° C. in an ice bath, 0.25 g of N-hydroxysuccinimide was added, and 2.1 mL of dichloromethane was added, and cooled to 0° C. DCC (0.44 g, dissolved ...

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Abstract

The invention discloses a technetium-99m labeled dimercaptopropanol amido new lactose albumin complex, a preparation method and application thereof; radioactive pertechnetate (TcO4) is synthesized with dimercaptopropanol amido new lactose albumin into a ligand (DMP-NGA); and under the presence of reducing agent and protective agent, the radioactive technetium-99m labeled dimercaptopropanol amido new lactose albumin complex is prepared by reaction. The complex has good chemical stability and biological property, high initial uptake value and target and chemical purity, simple preparation and low use cost, and can be used in radiopharmaceuticals and clinical nuclear medicine technology field as a novel liver imaging agent.

Description

Technical field [0001] The present invention relates to 99m The technical field of Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine, in particular relates to a technetium-99m-labeled dimercaptopropionamide-based neolactoalbumin complex and its preparation method and application. Background technique [0002] ASGP receptor (Asialoglycoprotein receptor, ASGP-R) is the abbreviation of asialoglycoalbumin receptor. a bit. Almost all plasma proteins except albumin are glycoproteins whose sugar chain ends with sialic acid when synthesized by the liver and released into the blood. Sialic acid forms weak linkages with other sugar groups, is unstable in the blood and is easily cleared. The sialic acid moiety is removed, marking the end of the glycoprotein's life. The galactose structure in most plasma proteins is located at the second position of the terminal, so when the terminal sugar is enzymatically hydrolyzed, the glycoprotein ending with galactose can s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/765C07K1/13A61K51/08A61K103/10
Inventor 张现忠杨文江牟甜甜王学斌唐志刚张俊波陆洁
Owner BEIJING NORMAL UNIVERSITY
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