PET (Positron Emission Tomography) tracer with FSHR (Follicle-stimulating Hormone Receptor) targeting as well as preparation method and application thereof
A tracer, targeting technology, applied in the field of PET tracer, can solve the problem of undetected, achieve the effects of rapid imaging, early detection, and rapid tissue penetration
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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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