[18F] DPA-714 (N, N-diethyl-2-(2-(4-(2-[18]F-fluoroethyoxy)phenyl)-5, 7-dimethylpyrazolo[1, 5-a]pyrimidin-3-yl)aceamide) derivative and preparation and application methods thereof

Abstract

The invention discloses a [18F] DPA-174 derivative. The [18F] DPA-174 derivative is prepared by modifying the benzene ring structure of or prolonging the carbon chain structure of a [18]F DPA-174 imaging agent. The invention also discloses preparation and application methods of the [18F] DPA-174 derivative. The [18F] DPA-174 derivative is simple in preparation, easy to implement, high in labellingyield and good in repeatability and can help in real time observe and in vivo monitor the status of intracerebral neuroinflammation of an animal model as well as the changes of the major organs and tissues of the animal model; the prepared imaging agents can achieve imaging effects on neuroinflammation; the [18F] DPAF imaging agent can achieve a high signal-to-noise ratio on neuroinflammation lesions to provide possibility for further monitoring and assessing the diagnosis and treatment effects on neuroinflammation..

Description

technical field [0001] The present invention relates to a class of 18 The F-labeled DPA-714 derivatives and their preparation method and application are mainly used for neuroinflammation state-specific imaging and belong to the field of medical diagnostic reagents. Background technique [0002] PET (Positron Tomography) utilizes nuclide labeling of positron emitters, such as some physiologically required compounds or metabolic substrates such as glucose, fatty acids, amino acids, receptor ligands, and water, etc. After being introduced into the body, positron scanning is applied In vivo radiological images obtained by machine. It has received extensive clinical attention for its ability to display the metabolic activity of organs or tissues and the function and distribution of receptors, also known as "in vivo biochemical imaging". It can be said that the emergence of PET has brought medical imaging technology to a new level, enabling non-invasive, dynamic and quantitative...

AI Technical Summary

Problems solved by technology

[0004] Invention purpose: to solve [ 18 F] DPA-714 imaging agent has problems such as low tumor uptake value, high non-specific binding, lower image signal-to-noise ratio, and unclear image display during the imaging process. [ 18 F] DPA-714 imaging agent is modified and transformed, increasing [ 18 F] the permeability of DPA-714 derivative imaging agent through the blood-brain barrier increases [ 18 F] The specific binding rate of the DPA-714 derivative imaging agent to the target increases [ 18 F] The utilization rate of DPA-714 derivative imaging agent in brain imaging makes derivatives more conducive to observing the specific imaging of neuroinflammation state in the brain of animal models; the [ 18 F] DPA-714 imaging agent is modified to generate new derivatives, and [ 18 F] DPA-714 imaging agent imaging comparison, found that some derivatives can improve the signal-to-noise ratio in animal model imaging, and have certain imaging advantages

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