A sort of 18 f-labeled guanidine methyl substituted benzene analogues and their applications

Abstract

The present invention provides a class of 18 F-labeled guanidinomethyl-substituted benzene analogues, the structure of which is shown in general formula 1, wherein the fluorinated polyethylene glycol chain is located at the para-position of the benzene ring and the guanidinemethyl-bonding position, n is 2-5, F for 18 F. of the present invention 18 F-labeled guanidinomethyl-substituted benzene analogs have the advantages of high radiochemical purity, good stability, high initial cardiac uptake, high target-to-non-target ratio, and long residence time, and can be used as a new type of fluorine-labeled PET cardiac nerve receptors. Volumetric imaging agents are used in the fields of radiopharmaceutical chemistry and clinical nuclear medicine.

Description

technical field [0001] The present invention relates to a 18 F-labeled guanidinomethyl-substituted benzene analogs and their applications. Background technique [0002] Cardiovascular disease seriously endangers human health. According to the World Health Organization, the mortality rate of cardiovascular disease in my country is significantly higher than that of Japan and developed countries in Europe and America. The incidence of cardiovascular disease in my country is still high and growing rapidly, and the incidence of acute and chronic cardiac ischemia, arrhythmia, heart failure and other heart diseases remains high. The impairment of the functional integrity of the autonomic nervous system (ANS) is closely related to the early pathogenesis and prognosis of common heart diseases such as acute and chronic myocardial ischemia and heart failure. Therefore, research on the evaluation and detection of the mechanism of ANS dysfunction in heart disease has important clinical...

AI Technical Summary

Problems solved by technology

[0007] However, 123 The clinical use of I-MIBG (especially in China) is severely limited due to the following reasons: (1) low spatial and temporal resolution, resulting in poor image quality; (2) lack of tissue attenuation correction It is not an effective method, so it cannot quantitatively evaluate the ANS function; (3) the initial uptake of the liver is high and the metabolism is slow, which affects the visualization of the heart; (4) obtaining nuclides in China 123 I am inconvenient and therefore not yet commercially available 123 I-MIBG

[0008] The high-resolution, high-sensitivity, high-accuracy and effective tissue attenuation correction method of PET imaging technology, especially the combined application of PET / CT, make cardiac PET tracers in myocardial hemodynamics and cardiac receptor function and There are clear advantages in terms of density evaluation, but 11 C-labeled positron cardiac sympathetic nerve imaging agents generally have disadvantages such as complicated preparation process, low yield, poor biological performance, and poor image quality.

also, 11 The C nuclide has a short half-life (T 1 / 2 =20.39min), need to configure on-site cyclotron, high production cost, and low inspection efficiency, do not use clinical promotion

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