18F marked methylguanidine substituted benzene analogue and application thereof

Abstract

The invention provides a 18F marked methylguanidine substituted benzene analogue, the structure is shown as in the general formula I, wherein a fluoro-polyethylene glycol chain is located on the para-position, bonded with guanidine methyl, of a benzene ring, n is 2-5, and F is 18F. The 18F marked methylguanidine substituted benzene analogue has the advantages of high radiochemical purity, good stability, high initial uptake value of heart, high ratio of target to non-target, long detention time and the like, and can be applied as a novel fluorine marked PET cardiac nerve receptor photographicdeveloper to the fields of radiopharmaceutical chemistry and clinic nuclear medicines.

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 is a serious threat to 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 clini...

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 ANS function; (3) the initial uptake in the liver is high and the metabolism is slow, which affects the visualization of the heart; (4) the nuclides are obtained domestically 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 tracer in myocardial hemodynamics and cardiac receptor function and There are clear advantages in terms of density evaluation, but 11 C-labeled positron cardiac nerve receptor imaging agents generally have disadvantages such as complicated preparation process, low yield, poor biological performance, and poor image quality.

also, 11 C nuclides have 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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