Application of berberine or derivatives thereof in preparation of myocardial perfusion imaging agent
The 18F-labeled berberine derivative solves the problems of the short half-life of the PET myocardial perfusion imaging agent nuclide and the inability to perform exercise stress imaging, and achieves the effect of high affinity and long-term maintenance of high radioactivity distribution in myocardial cells. , providing a new PET myocardial perfusion imaging agent suitable for clinical application.
Inactive Publication Date: 2017-10-10
WEST CHINA HOSPITAL SICHUAN UNIV
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Problems solved by technology
At present, there is no research report on the use of berberine or its derivatives in myocardial perfusion imaging
Method used
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Embodiment 1
[0040] Example 1 Preparation of 18F-labeled berberine derivatives of the present invention
[0041] 18F labeled berberine derivatives of the present invention (named as [ 18 F] HX-01) is provided by the Department of Nuclear Medicine, West China Hospital, Sichuan University, and can also be synthesized according to the patented method with the notification number CN 102989017B.
[0042] [ 19 F] HX-01: 18F-labeled berberine derivative non-radioactive reference substance, synthesized according to the patented method with the notification number CN102989017 B.
[0043] The beneficial effect of the present invention is specified below by test example:
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Abstract
The invention provides application of berberine or derivatives thereof in the preparation of a myocardial perfusion imaging agent. The invention further provides application of 18F labelled berberine or derivatives thereof in the preparation of the myocardial perfusion imaging agent. In-vitro researches, in-vivo biological distribution, small animal PED dynamic imaging and the like prove that the 18F labelled berberine derivatives can specifically gather in myocardial cells or heart tissue, has good cardiac muscle targeting distribution features in living animals, are high in heart / surrounding tissue (liver, lung, blood, muscles, bones and the like) comparison value, can be used as a good PET myocardial perfusion imaging agent and is promising in clinical application prospect.
Description
technical field [0001] The invention belongs to the field of medical diagnosis, and in particular relates to the use of berberine or its derivatives in the preparation of myocardial perfusion imaging agents. Background technique [0002] Coronary heart disease is one of the main diseases that endanger human survival and health. Statistics show that the morbidity and mortality of coronary heart disease in my country are increasing year by year, and it is developing towards a younger trend. It is not only the pain of patients, but also the family and society. heavy financial burden. Since the 1970s, myocardial perfusion imaging has been used for non-invasive diagnosis of heart disease, and it has become an important imaging method for diagnosing coronary heart disease, evaluating the degree and extent of coronary artery disease, evaluating curative effect and judging prognosis. Significance. [0003] Myocardial perfusion imaging is divided into SPECT (nuclear medicine single ...
Claims
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IPC IPC(8): A61K51/04A61K101/02C07D455/03
CPCA61K51/0455C07B2200/05C07D455/03
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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