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A sort of 68 Ga-labeled molecular probe, preparation method and application thereof

A molecular probe, 68ga technology, applied in the field of nuclear medicine imaging, achieves good stability, good application prospects, and excellent imaging effects

Active Publication Date: 2022-05-31
XIANGYA HOSPITAL CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the application of polyamine molecular probes in PET / CT imaging.

Method used

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  • A sort of <sup>68</sup> Ga-labeled molecular probe, preparation method and application thereof
  • A sort of <sup>68</sup> Ga-labeled molecular probe, preparation method and application thereof
  • A sort of <sup>68</sup> Ga-labeled molecular probe, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation method of the molecular imaging agent described in this embodiment is as follows:

[0033] 1) Put 25ug of the precursor compound NOTA-Spermin into the EP tube, add 1ml of 0.25M NaOAc solution, mix well and transfer to the reaction tube;

[0034] 2) with 4ml of 0.05M HCl solution 68 GaCl3 is rinsed into the reaction tube, after rinsing 68 The Ga radioactivity was 31mCi, and the reaction was carried out at 90 °C for 10 min. After the reaction, 10 ml of deionized water was added to quench the reaction;

[0035] 3) The solution in the reaction tube is enriched through the C18 Plus column, and the C18 Plus column is washed with 10 mL of deionized water; then the C18 Plus column is washed with 1 ml of ethanol and 10 ml of normal saline to obtain an eluent, and the eluent is passed through without After bacterial filtration membrane, it is loaded into the product bottle to obtain the imaging agent injection 68 Ga-NOTA-Spermin.

[0036] Imaging agent injecti...

Embodiment 2

[0041] The preparation method of the molecular imaging agent described in this embodiment is as follows:

[0042] 1) Put 30ug of the precursor compound NOTA-Spermidine into the EP tube, add 1ml of 0.25M NaOAc solution, mix well and transfer it to the reaction tube;

[0043] 2) with 4ml of 0.05M HCl solution 68 GaCl3 is rinsed into the reaction tube, after rinsing 68 The Ga radioactivity was 33mCi, and the reaction was carried out at 90 °C for 10 min. After the reaction, 10 ml of deionized water was added to quench the reaction;

[0044] 3) The solution in the reaction tube is enriched through the C18 Plus column, and the C18 Plus column is washed with 10 mL of deionized water; then the C18 Plus column is washed with 1 ml of ethanol and 10 ml of normal saline to obtain an eluent, and the eluent is passed through without After bacterial filtration membrane, it is loaded into the product bottle to obtain the imaging agent injection 68 Ga-NOTA-Spermidine.

[0045] Imaging agen...

Embodiment 3

[0050] The preparation method of the molecular imaging agent described in this embodiment is as follows:

[0051] 1) Put 30ug of the precursor compound NOTA-Putrescine into an EP tube, add 1ml of 0.25M NaOAc solution, mix well and transfer it to a reaction tube;

[0052] 2) with 4ml of 0.05M HCl solution 68 GaCl3 is rinsed into the reaction tube, after rinsing 68 The Ga radioactivity was 35mCi, and the reaction was carried out at 90 °C for 10 min. After the reaction, 10 ml of deionized water was added to quench the reaction;

[0053] 3) The solution in the reaction tube is enriched through the C18 Plus column, and the C18 Plus column is washed with 10 mL of deionized water; then the C18 Plus column is washed with 1 ml of ethanol and 10 ml of normal saline in turn to obtain an eluent, and the eluent is passed through without After bacterial filtration membrane, it is loaded into the product bottle to obtain the imaging agent injection 68 Ga- NOTA-Putrescine.

[0054] Imagin...

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Abstract

The invention relates to the technical field of nuclear medicine imaging, specifically a 68 Ga-labeled molecular probes, preparation methods and applications. The preparation methods include: 1) mixing the precursor compound with 0.25M NaOAc solution and placing it in a reaction tube; 2) using 0.05M HCl solution to 68 GaCl 3 Rinse into the reaction tube for reaction, after the reaction, add deionized water to quench the reaction; 3) enrich the solution in the reaction tube through the C18Plus column; then rinse the C18Plus column with ethanol and normal saline to obtain the leaching solution, and the eluent was passed through a sterile filter membrane to obtain molecular probe injection. obtained by the present invention 68 Ga-labeled molecular probes have good targeting and a high target-to-non-target ratio. They are applied to tumor PET / CT imaging with good effects, and the preparation conditions are mild and the steps are simple, which is conducive to clinical promotion and application. Application prospect.

Description

technical field [0001] The invention relates to the technical field of nuclear medicine imaging, in particular to a 68 Ga-labeled molecular probe, preparation method and application thereof. Background technique [0002] The early diagnosis of tumors is an important research content of molecular imaging, which can provide effective means for the effective treatment of tumors. The tumor diagnosis technology based on PET imaging has become an important tool for early diagnosis of tumors because of its high resolution, high tissue penetration, low dose, and real-time in vivo imaging. At present, there are two main design principles of PET-based tumor contrast agents: 1) abnormal tumor nutritional requirements; 2) tumor-specific highly expressed receptors. The way of recognition by receptors is more specific and the diagnostic efficiency is higher. However, the search, characterization, verification, and ligand design of receptors all require a lot of work, and the cost is hi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D255/02C07B59/00A61K51/04A61K49/04A61K103/00
CPCC07D255/02C07B59/004A61K51/044A61K49/04C07B2200/05
Inventor 胡硕周文虎周明朱泽华
Owner XIANGYA HOSPITAL CENT SOUTH UNIV
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