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PET (Polyethylene Terephthalate) imaging agent for targeting TREM2 receptor as well as preparation method and application of PET imaging agent

A PET imaging agent and receptor technology, applied in the field of PET imaging agents targeting TREM2 receptors and their preparation, can solve the problems of slow metabolism, high radiation dose, large molecular weight of imaging agents, etc. The effect of low radiation dose and excellent image quality

Pending Publication Date: 2021-10-22
ZHONGSHAN HOSPITAL FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a Ga-68-labeled PET imaging agent for TREM2 receptors and a preparation method thereof for the existing imaging agents with large molecular weight, slow metabolism, and high radiation dose to subjects. and its application in differentiating inflammation from tumor

Method used

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  • PET (Polyethylene Terephthalate) imaging agent for targeting TREM2 receptor as well as preparation method and application of PET imaging agent
  • PET (Polyethylene Terephthalate) imaging agent for targeting TREM2 receptor as well as preparation method and application of PET imaging agent
  • PET (Polyethylene Terephthalate) imaging agent for targeting TREM2 receptor as well as preparation method and application of PET imaging agent

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Synthesis of compound 1:

[0036]

[0037]1) Weigh MBHA resin (0.2mmol, 0.77g, sub:0.26mmol / g) into the solid phase tube, add DMF, and blow nitrogen for 2 hours;

[0038] 2) wash the resin three times with DMF;

[0039] 3) Add 20% piperidine / DMF, blow with nitrogen for 0.5h;

[0040] 4) wash the resin five times with DMF;

[0041] 5) Add Fmoc-protected amino acid to the above resin, add DMF solution and mix well, then add condensing agent and alkali in sequence, and react with nitrogen blowing for 1 h;

[0042] 6) According to the following amino acid feeding table, repeat the above operation to connect each amino acid in sequence.

[0043] Table 1 Amino Acid Feeding Table

[0044]

[0045]

Embodiment 2

[0047] Synthesis of NOTA-COG1410:

[0048]

[0049] 1) After drying the compound 1 resin, add cutting solution (2.5% Tis / 2.5% H2O / 2.5% DTT / / 92.5% TFA) and shake at room temperature for 5 hours;

[0050] 2) filter the resin and collect the filtrate;

[0051] 3) Slowly pour the above-mentioned filtrate into a cold isopropyl ether solution, and centrifuge with a 3000-rpm centrifuge to obtain the crude peptide;

[0052] 4) The crude peptide was washed twice with isopropyl ether, and then dried to obtain 50 mg of crude product.

[0053] The crude product was purified by reverse phase preparative HPLC (Eluent of 0.1% TFA H 2 O / CH 3 CN on C-18columnchromatography), the target fraction was collected and lyophilized to obtain the target compound NOTA-COG1410 (10.9 mg, 95.0% purity), which was a white solid. See Table 2 for the purification conditions of NOTA-COG1410.

[0054] Table 2 NOTA-COG1410 purification conditions

[0055]

[0056]

Embodiment 3

[0058] 68 Synthesis of Ga-NOTA-COG1410:

[0059] Towards 68 CaCl 3 Add 0.1mol / L NaOAc buffer solution and 100μg NOTA-COG1410 successively to the solution, and react at 80°C for 10min to obtain 68 Ga-NOTA-COG1410, the spectrum is as follows figure 1 shown.

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Abstract

The invention relates to a PET (Polyethylene Terephthalate) imaging agent 68Ga-NOTA-COG1410 for targeting a TREM2 receptor and a ligand compound of the PET imaging agent 68Ga-NOTA-COG1410. The invention further discloses a preparation method of the PET imaging agent and application of the PET imaging agent in the aspects of identification, verification and tumor. The PET imaging agent targeting the TREM2 receptor and the ligand compound of the PET imaging agent are novel in chemical structure, have the advantages of small molecular weight, fast metabolism and low radiation dose suffered by subjects, and can realize staging and differential diagnosis of tumors.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceutical chemistry, in particular to a PET imaging agent targeting TREM2 receptors and its preparation method and application. Background technique [0002] Positron Emission Tomography (PET) is currently the best imaging device for detecting the occurrence and development of tumors and diseases in vivo. It can realize high-resolution imaging of cell metabolism and function, and analyze the physiological, biochemical Non-invasive, three-dimensional, dynamic study of the process. PET examination relies on the metabolism and absorption of spectral or specific targeted positron imaging agents in target organs. 18 F-FDG is currently the most commonly used imaging agent for PET, but 18 F-FDG has disadvantages such as poor specificity, sometimes false positive or false negative, and inability to distinguish tumor from inflammation. therefore 18 F-FDG is a non-specific imaging agent, and the diffe...

Claims

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Application Information

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IPC IPC(8): A61K51/04A61K51/08C07K7/08G01T1/29
CPCA61K51/0482C07K7/08A61K51/08G01T1/2985
Inventor 程登峰石岱司展林卿玉石洪成
Owner ZHONGSHAN HOSPITAL FUDAN UNIV
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