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A Molecular Imaging Probe with Dendrimer as the Core and Its Application

A molecular imaging and dendrimer technology, applied in the direction of radioactive carriers, etc., can solve the problems that single-target molecular imaging cannot accurately reflect the biological process in vivo, false positives and false negatives in disease diagnosis, etc., to improve the detection efficiency, quality and stability. Good sex, the effect of reducing the possibility

Active Publication Date: 2018-01-16
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The occurrence and development of many diseases are not caused by changes in a single indicator, so single-target molecular imaging cannot accurately reflect biological processes in vivo, which can easily lead to false positives or false negatives in disease diagnosis

Method used

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  • A Molecular Imaging Probe with Dendrimer as the Core and Its Application
  • A Molecular Imaging Probe with Dendrimer as the Core and Its Application
  • A Molecular Imaging Probe with Dendrimer as the Core and Its Application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 Preparation of Single Target Molecular Imaging Probe

[0054] 1) Under nitrogen protection, dissolve substance IV (20 mg, 38.71 μmol) in dichloromethane-tetrahydrofuran mixed solvent (in which volume ratio V dichloromethane: V tetrahydrofuran = 3:1), then add triethylamine (40 mg, 395.3 μmol), the mixture was placed in an ice-water bath and stirred, and the following substance (106.3 mg, 387.1 μmol) was added:

[0055]

[0056] After reacting at 40-70°C for 8 hours, it was cooled to room temperature, separated and purified by HPLC preparative chromatography, and dried in vacuo to obtain the compound of structure V (41.5 mg, 73%, retention time: 9 min). V electrospray mass spectrometer ESI-MS result: m / z=1469.68 (V molecular formula is C 78 h 88 N 18 o 12 , the theoretical value is 1469.68).

[0057]

[0058] 2) Dissolve substance V (14.7 mg, 10 μmol) in dichloromethane-tetrahydrofuran mixed solvent (wherein the volume ratio of V 二氯甲烷 :V 四氢呋喃 =3:1)...

Embodiment 2

[0074] Example 2 Preparation of double / single-target molecular imaging probes

[0075] 1) Dissolve substance A2 (17.7mg, 10μmol) in dichloromethane-tetrahydrofuran mixed solvent (wherein the volume ratio V 二氯甲烷 :V 四氢呋喃 =3:1), then added triethylamine (40mg, 395.3μmol), the mixture was placed in an ice-water bath and stirred, and the following substance (12.6mg, 30μmol) was added:

[0076]

[0077] Reacted at 40-70°C for 8 hours, cooled to room temperature, separated and purified by HPLC preparative chromatography, and dried in vacuum to obtain the compound of structure B2 (5.9 mg, 26%, retention time: 12.2 min). Substance B2 electrospray mass spectrometry ESI-MS result: m / z=2153.02 (B2 molecular formula is C 109 h 132 N 28 o 20 , the theoretical value is 2153.02).

[0078]

[0079] 2) The obtained product B2 (21.5 mg, 10 μmol) was dissolved in 3 mL of boric acid buffer (pH 8.5); CY-NHS (39.9 mg, 40 μmol) was added, stirred at room temperature for 2 to 5 hours, sepa...

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Abstract

A molecular imaging probe with a dendrimer as the core and its application, by connecting four rigid arm molecules on the dendrimer IV and connecting different functional molecules, so as to obtain a low-steric hindrance multi-mode multi-target molecule image probe. The obtained probe has good stability and high imaging contrast. Study the synthesized molecular imaging probes, realize the active targeting of molecular imaging probes to lesion sites by linking targeting molecules and signaling molecules, realize its role in the preparation of drugs for the diagnosis and treatment of different tumor diseases by linking different targeting molecules application.

Description

Technical field: [0001] The invention relates to an imaging molecular imaging probe, in particular to connecting multiple rigid molecules on dendrimer IV and continuing to connect a type of coupled isotope 64 Cu is connected with infrared dye molecules as signal molecules, and antibodies or antibody fragments are used as targeting molecules to form molecular imaging probes with dual targeting and dual modes, single targeting and dual modes, dual targeting and single mode or single targeting and single mode. Background technique: [0002] Molecular imaging is a cutting-edge discipline that integrates advanced imaging technology with molecular biology technology, computer information processing technology and other disciplines to image at the molecular level. Compared with traditional medical imaging technology, molecular imaging can understand the occurrence and development of diseases and their mechanisms at the molecular level, and provide molecular level information for ea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/06
Inventor 王怡红钱坤李新辈魏术海
Owner SOUTHEAST UNIV
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