PET (Positron Emission Tomography) tracer with FSHR (Follicle-stimulating Hormone Receptor) targeting as well as preparation method and application thereof

A tracer and targeting technology, applied in the field of PET tracers, can solve the problems of non-detection and achieve rapid imaging, which is conducive to early detection and rapid tissue penetration

Active Publication Date: 2015-01-28
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Meanwhile, FSHR expression was not detected in benign inflamed tissues and adjacent normal tissues

Method used

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  • PET (Positron Emission Tomography) tracer with FSHR (Follicle-stimulating Hormone Receptor) targeting as well as preparation method and application thereof
  • PET (Positron Emission Tomography) tracer with FSHR (Follicle-stimulating Hormone Receptor) targeting as well as preparation method and application thereof
  • PET (Positron Emission Tomography) tracer with FSHR (Follicle-stimulating Hormone Receptor) targeting as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The PET tracer described in this example uses the bifunctional chelating agent MAA-NOTA as a linker to conduct positron nuclides ( 18 F) Marking, the specific steps include:

[0068] 1) Label the precursor NOTA-MAA-FSH 33-53 Preparation: Add 1ml (8mg, 11.6mmol) of 0.2M ammonium acetate solution containing MAA-NOTA to 0.2M ammonium acetate solution containing the polypeptide compound (6.8mg, 2.6mmol) of the amino acid sequence shown in SEQ.ID NO:1 solution at room temperature for 1 hour.

[0069] After the reaction, use preparative HPLC to purify, the conditions are as follows:

[0070] Preparative reverse phase C 18 Column (Xbridge, 19×150mm, Waters);

[0071] Waters2998 diode array UV detector;

[0072] BioScan radioactivity detector;

[0073] Waters2545 binary high pressure gradient pump;

[0074] The mobile phase is: A, acetonitrile solution containing 0.1% trifluoroacetic acid (TFA); B, aqueous solution containing 0.1% TFA;

[0075] Gradient elution: 5%A and...

Embodiment 2

[0104] The targeted FSHR PET tracer described in this example uses the bifunctional chelating agent MAA-DOTA as a linker to conduct positron nuclides ( 68 Ga) marking, the specific steps include:

[0105] 1) Labeling precursor DOTA-MAA-FSH 33-53 Preparation: Add 1ml (3.9mg, 5mmol) of 0.2M ammonium acetate solution containing MAA-DOTA to 0.2M acetic acid containing the polypeptide compound (8mg, 3.0mmol) of the amino acid sequence shown in SEQ.ID NO:1 ammonium solution at room temperature for 1 hour.

[0106] After the reaction, use preparative HPLC to purify, the conditions are as follows:

[0107] Preparative reverse phase C 18 Column (Xbridge, 19×150mm, Waters);

[0108] Waters2998 diode array UV detector;

[0109] BioScan radioactivity detector;

[0110] Waters2545 binary high pressure gradient pump;

[0111] The mobile phase is: A, acetonitrile solution containing 0.1% trifluoroacetic acid (TFA); B, aqueous solution containing 0.1% TFA;

[0112] Gradient elution: 5...

Embodiment 3

[0140] The linking group of the PET tracer targeting FSHR described in this example is a labeling prosthetic group 18 F-NPFP, the positron nuclide ( 18 F) Marking, the specific steps include:

[0141] 1) 18 Preparation of F solution: Accelerator-produced 18 After F was adsorbed by QMA, it was absorbed by 1mL crown ether K 222 / K 2 CO 3 (15mg / 3mg) acetonitrile / water (9:1 by volume) solution was eluted into the reaction tube, and acetonitrile was removed twice. The crown ether K 222 (4,7,13,16,21,24-hexaoxo-1,10-diazidobicyclo[8.8.8]-hexacane) was purchased from Sigma, and CRC-15R activity meter (CAP INTEC ) to measure the radiation dose as 200mCi.

[0142] 2) 18 Preparation of F-NPFP: the prepared in step 1) 18 F-solution was added to 1 mL of acetonitrile solution containing 5 mg of 2-bromo-propionic acid methyl ester, and reacted at 120° C. for 10 minutes. After cooling, add 1 mL of 1M tetrabutylammonium hydroxide aqueous solution containing 50 μL, react at 90°C for...

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Abstract

The invention relates to a PET (Positron Emission Tomography) tracer which is obtained by polypeptide which is marked by positron imaging nuclide and has FSHR (Follicle-stimulating Hormone Receptor) targeting as well as a preparation method of the PET tracer. The invention also discloses application of the PET tracer in the field of tumor living body monitoring. With the adoption of the PET tracer, the blank in the field of FSHR targeting positron tracers and the technical problem of carrying out horizontal living body monitoring on FSHR are solved, and therefore, the PET tracer is particularly suitable for diagnosis and curative effect monitoring on tumors with high expression of the FSHR.

Description

technical field [0001] The invention relates to a PET tracer obtained by labeling a polypeptide compound with follicle-stimulating hormone receptor targeting property with a positron nuclide, and its application in detecting tumors. Background technique [0002] Follicle-stimulating hormone (FSH) is a hormone secreted by the pituitary gland that can stimulate sperm production and egg cell maturation. It exerts biological functions by binding to the follicle-stimulating hormone receptor (FSHR) distributed in the gonads. The main function of FSH is to promote follicular maturation. Human follicle-stimulating hormone promotes the proliferation and differentiation of follicular granulosa cells, and promotes the growth of the entire ovary. Follicle-stimulating hormone is one of the most important hormones in both sexes. It helps to regulate a series of physiological processes related to development, growth, pubertal maturation and reproduction, especially in the physiological pr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/08
Inventor 杨敏严勇军徐宇平潘栋辉王立振陈飞
Owner JIANGSU INST OF NUCLEAR MEDICINE
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