Central Neurodegeneration Imaging Agent and Method of Preparing the Same

A method of preparing a central neurodegeneration imaging agent, comprising Fluorine-18 solution (F-18 solution) preparation step, F-18-α-syn3 solution preparation step, and F-18-α-syn3 solution formula step sequentially, wherein:

• the F-18 solution preparation step comprises:
• step 1:
• introducing an F-18 solution into a first cartridge, withdrawing an elution solution for rinsing the first cartridge, collecting the F-18 solution rinsed out by a first eppendorf, and measuring activity of the F-18 solution;
• step 2:
• repeating the rinsing of step 1 twice, collecting the F-18 solutions rinsed out by a second eppendorf and a third eppendorf, and measuring activities of the F-18 solutions respectively;
• step 3:
• withdrawing the F-18 solutions of the first eppendorf, the second eppendorf and the third eppendorf according to operation-required activity, introducing the F-18 solutions withdrawn into a first container, measuring the activities of the F-18 solutions in the first container, heating the first container until the first container is totally dry and free of the F-18 solutions;
• step 4:
• introducing an organic solvent into the first container, heating the first container until the first container is totally dry, and repeating step 4 three times;
• the F-18-α-syn3 solution preparation step comprises:
• step 5:
• introducing a precursor into the first container, blending the precursor therein, heating the first container, and measuring activity of the precursor therein;
• step 6:
• taking a tiny amount of a crude product out of the first container by suction, dropping the tiny amount of the crude product onto a first thin-layer chromatography (TLC) plate, inserting the first TLC plate vertically into an expansion slot containing an expansion solution to perform instant thin-layer chromatography (iTLC), and calculating labeling efficiency;
• step 7:
• introducing totally a crude product of an F-18-α-syn3 precursor solution obtained by heating the first container into an activated silica column and measuring residual activity of the first container;
• step 8:
• withdrawing an organic solvent for rinsing the silica column, collecting a plurality of rinsing solutions, and measuring the activity of the silica column and each of the rinsing solutions;
• step 9:
• taking a tiny amount of an end product with maximum activity out of the plurality of rinsing solutions of step 8 by suction, dropping the tiny amount of the end product onto a second TLC plate, inserting the second TLC plate vertically into an expansion slot containing an expansion solution to perform iTLC analysis, and calculating labeling efficiency;
• step 10:
• withdrawing the end products of the plurality of rinsing solutions with maximum activity respectively, introducing the end products withdrawn into a second container, heating and evaporating the end products in the second container to concentrate the end product, causing the end product to become 1 mL in volume;
• step 11:
• withdrawing ddH2O, introducing the double-distilled water withdrawn into the second container, measuring the activity of the double-distilled water in the second container, separating and purifying the end product with high-performance liquid chromatography (HPLC);
• step 12:
• collecting first and second separated-peak solution (having activity) test tubes separately according to the HPLC separated-peak retention time and activity, and measuring their activities respectively;
• step 13:
• withdrawing and introducing the ddH2O into the second separated-peak solution test tube to perform dilution and measuring the activity of the ddH2O therein;
• the F-18-α-syn3 solution formula step comprises:
• step 14:
• withdrawing and introducing the separated, purified and diluted solution of step 13 into an activated second cartridge and measuring radioactivity of the second cartridge;
• step 15:
• withdrawing an organic solvent for rinsing the second cartridge, collecting a plurality of rinsing solutions, and measuring the activities of the second cartridge and each of the rinsing solutions;
• step 16:
• selecting, taking by suction, and introducing the rinsing solution with maximum activity of step 15 into a first eppendorf and measuring its activity;
• step 17:
• sequentially taking by suction and introducing a surfactant, an organic solvent and a normal saline into the first eppendorf, blending the surfactant, the organic solvent and the normal saline to become an F-18-α-syn3 formula solution, observing a color of the F-18-α-syn3 formula a solution, and measuring its activity;
• and
• step 18:
• withdrawing the F-18-α-syn3 formula solution, filtering the F-18-α-syn3 formula solution with a microporous membrane, collecting and introducing an F-18-α-syn3 labeling finished product solution into the second eppendorf, and measuring its activity to prepare a imaging agent F-18-α-syn3, wherein the F-18-α-syn3 is (Z)-1-(2-(2-fluoroethoxy) ethyl)-3-((E)-3-(4-nitrophenyl) a llylidene) indolin-2-one, and the F-18-α-syn3 has a structural formula shown below: