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A 68ga-labeled exenatide-like compound and its preparation method and application

A technology for exenatide and compounds, which is applied in the field of exenatide-like compounds and their preparation, can solve the problems of high production and maintenance costs, cumbersome synthesis process, etc., and achieve low toxic and side effects, high sensitivity, and low liver uptake Effect

Active Publication Date: 2018-06-26
NANJING FIRST HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

18 F-FBEM-Cys 39 -The synthesis process of exendin-4 is extremely cumbersome and takes more than 120 minutes
"Preliminary evaluation of [ 18 F]AlF-NOTA-MAL-Cys 39 -exendin-4in insulinoma with PET" discloses a simplified synthesis method using the chelating agent NOTA-MAL and Cys 39 Synthesis of NOTA-MAL-Cys by -exendin-4 reaction 39 -exendin-4, again by Al 18 F line one-step labeled synthesis [ 18 F]AlF-NOTA-MAL-Cys 39 -exendin-4, micro-PET imaging shows that the tumor site is radioactively concentrated and has a good target-to-background ratio, but its labeling yield is only 17.5±3.2%, and 18 F must be produced by a cyclotron, and the production and maintenance costs are high

Method used

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  • A 68ga-labeled exenatide-like compound and its preparation method and application
  • A 68ga-labeled exenatide-like compound and its preparation method and application
  • A 68ga-labeled exenatide-like compound and its preparation method and application

Examples

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Effect test

Embodiment 168

[0035] Example 1 68 Ga-NOTA-MAL-Cys 39 -Preparation of exendin-4

[0036] The present invention relates to experimental instruments and materials: 68 Ge / 68 Ga generator (German ABX company), 2480WIZARD2 automatic gamma counter (U.S. PerkinElmer company), high performance liquid chromatograph LC-20AT (Japan Shimadzu company); 30% Ultrapure hydrochloric acid (Germany Merck Gmbh), sodium acetate (U.S. Sigma), Sep-Pack C18 cartridge (Waters, USA), Physiological Saline (China Otsuka Pharmaceutical Co., Ltd.), NOTA-MAL-Cys 39 -exendin-4(> 98%, provided by Jiangsu Institute of Atomic Medicine, you can also refer to the document "Preliminary evaluation of[ 18 F]AlF-NOTA-MAL-Cys 39 -exendin-4in insulinoma with PET" preparation; absolute ethanol (Merck KGaA, Germany), micro-PET / CT (Siemens, Germany).

[0037] Use a 5ml syringe to extract 4mL of 0.05M HCl to rinse the germanium-gallium generator at a flow rate of 1mL / min while collecting the effluent; take 1ml of sodium acetate (0.25M) buffer...

Embodiment 268

[0040] Example 2 68 Ga-NOTA-MAL-Cys 39 -exendin-4 micro-PET / CT imaging in tumor-bearing mice

[0041] (1) Immunocytochemical staining

[0042] Insulinoma cells (INS-1 cells) press 5×10 5 / Well density is spread on a 24-well plate, placed in an incubator and incubated overnight. The next day, use a pipette to remove the culture medium in the wells, and fix the cells with 95% ethanol for 30 minutes after rinsing with PBS, and then rinse with PBS. After adding hydrogen peroxide to react at room temperature for 5 minutes, rinse with PBS, and then add the primary antibody (1:200 mouse anti-human GLP-1). In the negative control group, PBS was used instead of the primary antibody and placed at 37℃ for 1 hour. After rinsing with PBS, add secondary antibody (rabbit anti-rat IgG-HRP) at 37°C for 15 minutes. After PBS rinsing, diaminobenzidine (DAB) was added for color development, reacted for 3 minutes, washed with PBS, stained with hematoxylin, washed, and inspected under microscope. Aft...

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Abstract

The invention discloses <68>Ga marked NOTA-MAL-Cys<39>-exendin-4 compound as well as a preparation method and application thereof. The <68>Ga-NOTA-MAL-Cys<39>-exendin-4 is prepared from <68>Ga marked precursor compound of NOTA-MAL-Cys<39>-exendin-4. Synthesizing time of the <68>Ga-NOTA-MAL-Cys<39>-exendin-4 disclosed by the invention is about 25min, a labeling yield is as high as 80% or more, HPLC determination shows that a product radiochemical purity is larger than 98%, and the marked product of the <68>Ga-NOTA-MAL-Cys<39>-exendin-4 can be specifically combined with glucagon-like peptide-1 receptor (GLP-1R), is a GLP-1 receptor photographic developer having potential and is suitable for being applied to clinical insulinoma diagnosis.

Description

Technical field [0001] The invention belongs to the technical field of radionuclide labeling, and specifically relates to a 68 Ga-labeled exenatide-like compounds and preparation methods and applications thereof. Background technique [0002] Insulinoma, also known as pancreatic β-cell tumor, is a common type of pancreatic neuroendocrine tumors, which can cause hyperinsulinemia and cause symptoms such as hypoglycemia. Surgical treatment is the only radical cure for insulinoma, and precise positioning before surgery is the key to surgical treatment. Because insulinomas are small (usually less than 1-2cm), routine imaging examinations may be missed. Angiography and selective arterial calcium stimulation venous blood sampling to determine insulin (ASVS) can increase the detection rate, but it is invasive Check, there are risk factors such as infection and bleeding. High-precision and non-invasive tumor positioning methods have become a research hotspot in recent years. [0003] At ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/575C07K1/13A61K51/08A61K103/00
CPCA61K51/08C07K14/57563
Inventor 王峰杨敏张朋俊潘栋辉徐宇平
Owner NANJING FIRST HOSPITAL
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