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Technetium-99m marked 6-hydrazino pyridine-3-formamido novel lactose albumin complexes, preparation and use thereof

A technology of hydrazinopyridine and -99m, which is applied in the field of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of slow liver clearing and low non-target organ uptake, and achieve the effect of high ratio, simple preparation and low cost of use

Inactive Publication Date: 2011-10-12
BEIJING NORMAL UNIVERSITY +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Japanese scholars reported that using tricine as a donor ligand, the resulting complex 99m Tc-tricine / HYNIC-NGA has good in vivo stability and low non-target organ uptake. Although it can be used as a potential liver receptor imaging agent, it also has the disadvantage of slow clearing in the liver

Method used

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  • Technetium-99m marked 6-hydrazino pyridine-3-formamido novel lactose albumin complexes, preparation and use thereof
  • Technetium-99m marked 6-hydrazino pyridine-3-formamido novel lactose albumin complexes, preparation and use thereof
  • Technetium-99m marked 6-hydrazino pyridine-3-formamido novel lactose albumin complexes, preparation and use thereof

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Embodiment Construction

[0036] The present invention is described in detail below through examples, a technetium-99m-labeled 6-hydrazinopyridine-3-carboxamide-based neolactoalbumin complex:

[0037] (1) Preparation of ligand HYNIC-NGA:

[0038] HCl gas was passed through dioxane at an appropriate rate for 10 minutes to obtain a solution of HCl in dioxane. Dissolve 100mg of succinimide-6-tert-butoxycarbonylhydrazinopyridine-3-carboxylic acid in 2mL of dioxane, add 2mL of HCl / dioxane after all dissolved, and stir the reaction at room temperature mixture. After 5 minutes, the solution became cloudy and a precipitate formed. Stirring was continued in the dark for 4 hours. The turbid reaction mixture was filtered, and the solid was washed repeatedly with ether to obtain 55 mg of a white solid. Yield 67%.

[0039] Weigh 100 mg of NGA and dissolve it in 5 mL of 0.2 mol / L pH8.6 boric acid buffer at a concentration of about 20 mg / mL. Succinimid-6-ylhydrazinopyridine-3-carboxylic acid (6.5 mg dissolved i...

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Abstract

The invention discloses a technetium-99m labeled 6-hydrazino-pyridine-3-formyl amino lactose albumin new complex, a preparation method and application thereof. The complex takes N-hydroxyethyl-ethylenediamine-N, N', N'-triacetic acid (HEDTA) as a co-ligand, and under the presence of co-ligand and reducing agent, the radioactive technetium-99m labeled 6-hydrazino-pyridine-3-formyl amino lactose albumin new complex is prepared by reaction when the 6-hydrazino-pyridine-3-formyl amino new lactose albumin is matched. The complex has good chemical stability and biological property, high initial uptake value and target and non-target ratio, 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 6-hydrazinopyridine-3-carboxamide-based neolactoalbumin complex, its preparation method and application. Background technique [0002] In the technical field, the asialoglycoprotein receptor, referred to as ASGP receptor (Asialoglycoprotein receptor, ASGP-R), exists on the membrane of mammalian liver cells, and mediates the liver to remove asialoglycoprotein (Asialoglycoprotein) in the blood. , the specific site of ASGP). 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 galacto...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/765C07K1/13A61K51/08A61K103/10
Inventor 张现忠杨文江牟甜甜王伟平庞燕王学斌唐志刚陆洁张俊波
Owner BEIJING NORMAL UNIVERSITY
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