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Exendin-4 radioactive probe targeting a glucagon-like peptide-1 receptor, and preparation method thereof

A mal-cys39-exendin-4, ga-hbed-cc-mal-cys39-exendin-4 technology, which is applied in the field of exendin-4 radioactive probe and its preparation, can solve the problem of high non-specific uptake in kidney, pancreatic islet beta cells Low specific uptake and other problems, to achieve the effect of good in vivo biological metabolism, high specificity and high affinity

Active Publication Date: 2021-06-25
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, the probes reported so far all have problems such as low specific uptake by pancreatic β cells and high non-specific uptake by the kidney, so there is a lot of room for improvement

Method used

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  • Exendin-4 radioactive probe targeting a glucagon-like peptide-1 receptor, and preparation method thereof
  • Exendin-4 radioactive probe targeting a glucagon-like peptide-1 receptor, and preparation method thereof
  • Exendin-4 radioactive probe targeting a glucagon-like peptide-1 receptor, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 ([ 68 Ga]Ga-HBED-CC-MAL-Cys 39 -exendin-4)

[0044] step 1: 68 Synthesis of Ga-labeled Labeled Precursor of Exendin-4 Radioactive Probe Targeting Glucagon-Like Peptide-1 Receptor

[0045] HBED-CC-MAL-Cys 39 -exendin-4 is N,N'-bis[2-hydroxy-5-(carboxyethyl)-benzyl]ethylenediamine-N,N'-diacetic acid-N-ethylsuccinimide-(semi cystine-proline-proline-proline-alanine-glycine-serine-serine-proline-glycine-glycine-asparagine-lysine-leucine-tryptophan- Glutamic acid-Isoleucine-Phenylalanine-Leucine-Arginine-Valine-Alanine-Glutamic Acid-Glutamic Acid-Glutamic Acid-Methionine-Glutamine-Lysine acid-serine-leucine-aspartic acid-serine-threonine-phenylalanine-threonine-glycine-glutamic acid-glycine-histidine) synthesis;

[0046] Synthetic reaction equation:

[0047]

[0048] resolve resolution:

[0049] The compound 3,3'-(((2,2,13,13-tetramethyl-4,11-dioxo-3,12-dioxa-6,9-diazatetradecane-6,9 -Diyl)bis(methylene))bis(4-hydroxy-3,1-phenylene))dipropionic acid (64 ...

Embodiment 2

[0064] Embodiment 2 ([ 68 Ga]Ga-HBED-CC-Di(MAL-Cys 39 -exendin-4) synthesis)

[0065] step 1: 68 Synthesis of Ga-labeled Labeled Precursor of Exendin-4 Radioactive Probe Targeting Glucagon-Like Peptide-1 Receptor

[0066] HBED-CC-Di(MAL-Cys 39 -exendin-4), that is, N,N'-bis[2-hydroxy-5-(carboxyethyl)-benzyl]ethylenediamine-N,N'-diacetic acid-bis[N-ethylsuccinyl Amine-(cysteine-proline-proline-proline-alanine-glycine-serine-serine-proline-glycine-glycine-asparagine-lysine-leucine- Tryptophan-Glutamic Acid-Isoleucine-Phenylalanine-Leucine-Arginine-Valine-Alanine-Glutamic Acid-Glutamic Acid-Glutamic Acid-Methionine-Glutamine Amide-lysine-serine-leucine-aspartic acid-serine-threonine-phenylalanine-threonine-glycine-glutamic acid-glycine-histidine)] synthesis;

[0067] Synthetic reaction equation:

[0068]

[0069] resolve resolution:

[0070] The compound 3,3'-(((2,2,13,13-tetramethyl-4,11-dioxo-3,12-dioxa-6,9-diazatetradecane-6,9 -Diyl)bis(methylene))bis(4-hydroxy-3,1...

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Abstract

The invention relates to an exendin-4 radioactive probe targeting a glucagon-like peptide-1 receptor, and a preparation method thereof, and belongs to the field of radiopharmaceutical chemistry. The structural formula of the radioactive probe is shown in the specification. The marking time of the radioactive probe is 8 min, and the marking yield is more than 99%, the radiochemical purity the product, determined by radio-HPLC is more than 99%. The product shows high affinity and high specificity to the glucagon-like peptide-1 receptor, meanwhile, has better in-vivo biological metabolism property, and is a potential PET imaging agent for the glucagon-like peptide-1 receptor.

Description

technical field [0001] The invention relates to an exendin-4 radioactive probe targeting glucagon-like peptide-1 receptors and a preparation method thereof, belonging to the technical field of radiopharmaceutical chemistry. Background technique [0002] In recent years, the prevalence of diabetes in my country has been increasing rapidly. "Guidelines for the Prevention and Treatment of Type 2 Diabetes in China" (2020 Edition) shows that the prevalence of diabetes in my country is gradually increasing: 9.1% in 2010, 10.4% in 2013, and 11.2% in 2017. At present, the number of diabetic patients in China has reached 116.4 million, accounting for a quarter of the total number of patients in the world, ranking first in the world (International Diabetes Atlas, 2019). Diabetes has become the second largest chronic disease after hypertension, and its complications have brought serious disease burden and social burden to the people of our country. Early detection and early treatment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575C07K1/13A61K51/08A61K103/00
CPCC07K14/57563A61K51/08Y02P20/55
Inventor 朱霖李林璘赵睿玥孔繁渊
Owner BEIJING NORMAL UNIVERSITY
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