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MRI molecular image probe and preparing method thereof

A technology of molecular imaging and probes, which is applied in the analysis of materials, material analysis through resonance, sensors, etc., can solve the problems of unstable specificity, poor penetration and permeability, and increase the complexity of synthesis, so as to improve the penetration Sex, good use effect, effect of improving biological performance

Inactive Publication Date: 2009-02-11
PEOPLES HOSPITAL PEKING UNIV
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Problems solved by technology

Compared with PET technology, nuclear magnetic resonance imaging molecular imaging technology has the advantages of non-radioactive probes and high anatomical resolution of images; but the disadvantage is low signal detection and specificity
This is mainly due to the following problems in antibodies and specific monoclonal antibody probes: antibodies need to be desensitized when used; antibodies, including specific monoclonal antibodies, are still unstable in vivo, and it is difficult to meet expectations The purpose; the antibody has a large molecular weight and poor penetration and permeability in the tissue, so the best imaging time is long
This obviously increases the complexity of synthesis and the cost of making the probe, making the MRI probe lose the value of actual clinical use

Method used

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  • MRI molecular image probe and preparing method thereof
  • MRI molecular image probe and preparing method thereof
  • MRI molecular image probe and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Embodiment 1, HYNIC and Tricine and the MRI probe of paramagnetic metal Gd

[0042] 1. GdCl 3 Synthesis: take 36.3mg Gd 2 o 3 , add 10ml of 0.1mol / L HCl, and heat to 60°C. Continue to react for 10 minutes until it is completely dissolved, then heat to 100°C to evaporate excess HCl.

[0043] 2. Preparation of chelating agent solution: 3 mg [HYNIC-D-Phe 1 ,Tyr 3 ]-Octreotide (HYNIC-TOC, synthesized by Shanghai Gil Biochemical Company) was dissolved in 8ml0.2M Na 2 HPO 4 In PH6-7 buffer solution, take 20mg Tricine and 50mg mannitol after fully dissolving in the above solution, and heat in a water bath for 10 minutes.

[0044] 3. Preparation of MRI probe: take the GdCl synthesized in the first step 3 (3-4 μmol) was added to the above-mentioned chelating agent solution for chelating reaction, shaken and mixed at room temperature, and the product was separated by HPLC to obtain the Gd-Tricine-HYNIC-Octreotide molecular probe.

[0045] The molecular weight of the mole...

Embodiment 2

[0054] Embodiment 2, HYNIC and EDDA and the MRI probe of paramagnetic metal Gd

[0055] 1. GdCl 3 Synthesis: take 36.3mg Gd 2 o 3 , add 10ml of 0.1mol / L HCl, and heat to 60°C. Continue to react for 10 minutes until it is completely dissolved, then heat to 100°C to evaporate excess HCl.

[0056] 2. Prepare chelating agent solution: mix 3mg [HYNIC-D-Phe 1 ,Tyr 3 ]-Octreotide (HYNIC-TOC) dissolved in 8ml 0.2M Na 2 HPO 4 In PH6-7 buffer solution, after fully dissolving, take 40mg EDDA and 50mg mannitol and dissolve them in the above solution, and heat in a water bath for 10 minutes.

[0057] 3. Preparation of MRI probe: take the GdCl synthesized in the first step 3 (3-4 μmol), added to the above-mentioned chelating agent solution for chelating reaction, shaken and mixed at room temperature, and the product was separated by HPLC to obtain Gd-EDDA-HYNIC-Octreotide molecular probe.

[0058] Through animal experiments, it has the same performance as the Gd-Tricine-HYNIC-Octre...

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Abstract

A MRI molecular image probe with high biologic performance and low cost is composed of central ion, specific molecule and chelating agent consisting of primary chelating agent chosen from HYNIC and secondary one chosen from Tricine and EDDA. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to an MRI molecular imaging probe and a synthesis and preparation method thereof. Background technique [0002] Magnetic resonance imaging (MRI) technology is one of the three major technologies of medical molecular imaging, and others include PET (SPECT) and optical imaging. Compared with PET technology, nuclear magnetic resonance imaging molecular imaging technology has the advantages of non-radioactive probes and high anatomical resolution of images; however, the disadvantages are low signal detection and specificity. At present, MR is still in the category of anatomical morphology diagnosis. Functional MR and MR spectroscopy can only be classified into the early stage of indirect molecular imaging. MR molecular imaging has the potential to become the most promising molecular imaging method. What is lacking now is the direct molecular imaging method. Targeted specific probes. [0003] Probes are the basis of magnetic resonanc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61B5/055G01R33/20
Inventor 杜湘珂霍天龙张森李绪斌
Owner PEOPLES HOSPITAL PEKING UNIV
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