Preparation method of technetium labeled pyrroloquinoline quinone dimethyl ester
A technology of quinoline quinone dimethyl ester and dimethyl ester, which is applied in the field of biotechnology and medicine, and can solve the problems of affecting the amount of brain intake and large water solubility
Inactive Publication Date: 2011-06-15
JIANGSU INST OF NUCLEAR MEDICINE
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A document [YanyanKong, JRadioanalNuclChem, 2010] reported that PQQ was used as a ligand to complex with 99mTc to study the changes of N-methyl-D-aspartic acid (NMDA) receptors, but its water solubility is relatively large, which affects its entry into the brain. quantity
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Abstract
The invention provides a preparation method of technetium labeled pyrroloquinoline quinone dimethyl ester, belonging to the fields of biotechnology and medicine. By the preparation method, the structure of pyrroloquinoline quinone (PQQ) is modified, and PQQ-Z is prepared; and 99mTc labeling is carried out, and 99mTc-PQQ-Z is prepared. The product 99mTc-PQQ-Z has high radiochemical purity; and compared with the 99mTc-PQQ, the lipid / water partition coefficient of the 99mTc-PQQ-Z is increased from 1.49 to 0.67, the electrical property of the 99mTc-PQQ-Z is changed from anion electrical property to electric neutrality, and the brain entering amount of the 99mTc-PQQ-Z is twice of that of the 99mTc-PQQ.
Description
A kind of preparation method of technetium-labeled pyrroloquinoline quinone dimethyl ester technical field The invention discloses a preparation method of technetium-labeled pyrroloquinoline quinone dimethyl ester, which belongs to the fields of biotechnology and medicine. Background technique Pyrroloquinolinequinone (PQQ) is a new oxidoreductase prosthetic group discovered in the late 1970s. Its molecule has a planar conjugated molecular structure, conjugated diquinone (orthoquinone) and polyanions (three carboxyl groups). Pyrroloquinone quinone has a protective effect on neuroactivity, has an inhibitory effect on amyloid plaques, and also has a modulatory effect on N-methyl-D-aspartate receptor (NMDAR)-mediated excitotoxicity, and As a potential drug for the treatment of geriatric diseases, it has aroused the interest of neuroscience workers. A document [YanyanKong, JRadioanalNuclChem, 2010] reported that PQQ was used as a ligand to complex with 99mTc to study the chan...
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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
Inventor 周杏琴孔艳艳张建康曹国宪
Owner JIANGSU INST OF NUCLEAR MEDICINE
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