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Exenatide <18>F marker, and preparation method and application thereof

A marker, 18F technology, applied in the preparation method of peptides, chemical instruments and methods, peptides, etc., can solve the problems of not being able to know the labeling site and affect the diagnosis, and achieve high labeling efficiency, clear image contrast, and broad prospects Effect

Active Publication Date: 2014-10-22
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, it is recorded in Chinese patent CN102617728A that 18 The method of F-SFB labeling Exendin-4, but because the Exenatide sequence has 2 lysines, it is used 18 The way of F-SFB labeling cannot know the accurate labeling site, which will affect the later diagnosis

Method used

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  • Exenatide &lt;18&gt;F marker, and preparation method and application thereof
  • Exenatide &lt;18&gt;F marker, and preparation method and application thereof
  • Exenatide &lt;18&gt;F marker, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0049] Described in this example 18 F-FBEM-Cys 39 -The preparation of Exenatide marker comprises the following steps:

[0050] (1) Prepared by cyclotron 18 f - , and added to 0.1ml containing K 2 CO 3 (3mg) and Kryptofix 222 (15 mg) in a reaction flask of acetonitrile-water solution, by azeotropic evaporation to obtain anhydrous 18 f - ; take anhydrous 18 f - Add 4-trimethylamine ethyl benzoate trifluorosulfonate (5 mg, dissolved in 0.3 ml anhydrous dimethyl sulfoxide (DMSO)), heat to 115 ° C for 20 min, after cooling the reaction solution, then add 0.1 M NaOH for hydrolysis After acidification with 1M HCl; the reaction solution was purified by an activated Sep-Pak C18 column, and the product was rinsed with dichloromethane and dried with nitrogen to obtain 4- 18 F-benzoic acid;

[0051] (2) Take the prepared 4- 18 F-benzoic acid, add 0.3ml of DMSO solution containing 15mg2-aminoethylmaleimide, 10mg N, N-diisopropylethylamine (DIEA) and 20μL diethyl cyanophosphate,...

experiment example

[0059] 1. Small animal PET imaging of nude mouse model

[0060] Insulinoma INS-1 nude mice bearing GLP-1 receptor positive expression were placed on small animal PET beds, anesthetized with isoflurane, and fixed with adhesive tape. Model mice were injected with the labeled product obtained in Example 1 through the tail vein, 18 F-FBEM-Cys 39 - Exenatide in saline solution (1.85 MBq, 0.2 mL). 30 minutes, 1 hour, and 2 hours after injection, microPET imaging was performed, and the results were as follows: Figure 2A As shown, the arrow in the figure indicates the tumor.

[0061] As a comparison, another INS-1 nude mouse with insulinoma positive for GLP-1 receptor expression was placed on a small animal PET bed, anesthetized with isoflurane, and fixed with adhesive tape. Model mice were injected with the labeled product obtained in Comparative Example 1 through the tail vein, 18 F-FBEM-Cys 40 - Exenatide in saline solution (1.85 MBq, 0.2 mL). MicroPET imaging was performed...

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PUM

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Abstract

The invention belongs to the field of radioactive drug markers, and concretely relates to a <18>-FBEM-Cys39-Exenatide marker, and a preparation method and an application thereof. The 39th serine (Ser39) at the N-terminal of Exenatide is replaced by cysteine (Cys39) to obtain a novel Exenatide analog, and the specific combination characteristic of the mercapto group of the analog and a marking prosthetic group (<18>-FBEM) is used to realize the positioning marking of Exenatide. Preclinical researches show that the marked product <18>-FBEM-Cys39-Exenatide can be specifically combined with a GLP-1 receptor, is a latent GLP-1 receptor developer, and is suitable for diagnosing insulinoma.

Description

technical field [0001] The invention belongs to the field of radiopharmaceutical labeling, in particular to an exenatide 18 F marker and its preparation method and application. Background technique [0002] Insulinoma (Insulinoma), also known as pancreatic β-cell tumor, is a disease characterized by episodic hypoglycemia syndrome caused by the secretion of large amounts of insulin, and is a common cause of organic hypoglycemia. 90% of the tumors are located in the pancreas, and the probability of occurrence in the head, body, and tail of the pancreas is basically the same. There are risks of complications in invasive examinations such as celiac arteriography and percutaneous hepatic puncture through the portal vein system to draw blood and measure insulin in segments. Since the average diameter of insulinomas is less than 2cm, and the diagnostic sensitivity of conventional CT or MRI is only 50-70%, the non-invasive diagnosis of insulinomas often has deviations. like metho...

Claims

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Application Information

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IPC IPC(8): C07K14/575C07K1/20C07K1/13A61K51/08
CPCA61K51/08C07K14/575
Inventor 杨敏徐宇平潘栋辉王立振杨润琳陈飞许清朱晨
Owner JIANGSU INST OF NUCLEAR MEDICINE
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