Preparation method and application of 99mtc-labeled targeting tspo novel ligand cb86
A technology of 99mtc-cb86-dtpa and CB86-DTPA is applied in the field of preparation of 99mTc-labeled targeting TSPO new ligand CB86, which can solve the problems of low inspection cost, expensive PET equipment, and high inspection cost, and achieve the effect of low inspection cost
Active Publication Date: 2019-01-11
ZHONGSHAN HOSPITAL XIAMEN UNIV
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[0002] At present, most molecular imaging probes targeting TSPO are 18 Line PET imaging of F's markers, such as: 18 F-FEDAC, etc., but the PET equipment is expensive and the inspection cost is high, while the SPECT equipment is cheap, widely used, and the inspection fee is low. Therefore, it is extremely important and meaningful to develop molecular imaging probes targeting TSPOSPECT imaging.
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[0019] this invention 99m The preparation method of Tc-labeled targeting TSPO new ligand CB86 is to add the mixture agent DTPAA to the reagent CB86 dissolved in dimethyl sulfoxide, stir evenly at room temperature, and react for several days, then add ddH 2 O, make CB86-DTPA; then add PBS buffer and freshly prepared SnCl to CB86-DTPA 2 , shake well, after 10 minutes at room temperature, add fresh 99m TCO 4 - The solution was placed in a shaking module at 100°C for 10 minutes, cooled to room temperature, and purified by a C18 column to obtain 99m Tc-CB86-DTPA. Reagent CB86 is a biochemical test reagent CB86 with molecular formula C26H43NO3.
[0020] Specifically, the purity of CB86-DTPA>80% is obtained, that is, 99m The radioactive purity of Tc-CB86-DTPA was >90%.
[0021] to be more specific 99m The radioactivity concentration of Tc-CB86-DTPA is 2.9MBq / nmol.
[0022] Specifically, the mixture agent DTPAA was added to the reagent CB86 dissolved in dimethyl sulfoxide, st...
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The invention relates to a preparation method and application of 99mTc marked targeted TSPO novel ligand CB86. The preparation method and application aim at solving the problems that PET equipment is expensive and high in inspection charge. The method comprises the steps that a chelating agent DTPAA is firstly added into a reagent CB86 dissolved in dimethyl sulfoxide, the mixture is stirred to be uniform at room temperature, and after reacting is carried out for several days, ddH2O is added, and CB86-DTPA is prepared; then a pbs buffer solution and newly prepared SnCl2 are added into CB86-DTPA, the mixture is shaken up and is placed at room temperature for 10 minutes, then a fresh 99mTcO4-solution is added, the mixture is placed in a 100 DEG C oscillation module to react for 10 min, the product is cooled to room temperature and purified through a C18 small column, and 99mTc-CB86-DTPA is obtained. According to application, prepared 99mTc-CB86-DTPA is applied to an SPECT molecular image probe. The advantages of being suitable for SPECT equipment and low in inspection charge are achieved.
Description
technical field [0001] The invention relates to a molecular imaging probe targeting TSPO SPECT imaging, in particular to a 99m The preparation method and application of Tc-labeled targeting TSPO novel ligand CB86. Background technique [0002] At present, most molecular imaging probes targeting TSPO are 18 Line PET imaging of F's markers, such as: 18 F-FEDAC, etc., but PET equipment is expensive and the inspection cost is high, while SPECT equipment is cheap, widely used, and the inspection fee is low. Therefore, it is extremely important and meaningful to develop molecular imaging probes targeting TSPOSPECT imaging. Contents of the invention [0003] The purpose of the present invention is to overcome the above-mentioned defects of the prior art, to provide a kind of suitable SPECT equipment, the inspection cost is lower 99m The invention relates to a preparation method of Tc labeling targeting TSPO novel ligand CB86, and the invention also relates to its application. ...
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IPC IPC(8): C07D471/04C07B59/00A61K51/04A61K103/10
CPCA61K51/025A61K51/0455C07B59/002C07B2200/05C07D471/04
Inventor 苏新辉刘鹏郭志德张现忠
Owner ZHONGSHAN HOSPITAL XIAMEN UNIV