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PET tracer agent of targeted CBR receptor and preparation method and application of PET tracer agent

A tracer and targeting technology, which is applied in the field of radiopharmaceuticals and nuclear medicine, can solve the problems of low spatial resolution and inability to accurately locate the lesion, and achieve the effect of making up for technical vacancies

Pending Publication Date: 2022-04-26
ZHEJIANG UNIV
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Problems solved by technology

However, PET imaging also has its inherent shortcomings, which has low spatial resolution and cannot accurately locate the lesion.
[0004] Although 18-fluoro-deoxyglucose (18F-FDG), 18 The application of F-NaF in cancer has been increasingly promoted, but 18-fluoro-deoxyglucose (18F-FDG), 18 Most of the current clinical applications such as F-NaF are non-specific tracers, and it is difficult to perform specific imaging on specific regions or tissues

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  • PET tracer agent of targeted CBR receptor and preparation method and application of PET tracer agent
  • PET tracer agent of targeted CBR receptor and preparation method and application of PET tracer agent
  • PET tracer agent of targeted CBR receptor and preparation method and application of PET tracer agent

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Embodiment Construction

[0026] The technical solutions of the present invention will be further described below in conjunction with the accompanying drawings and specific examples. If the raw material used in the present invention, equipment are not specified otherwise, then all are known products, can obtain by commercially available products.

[0027] Compound SQKJ-1 and PET tracer 18 A preparation method of F-SQKJ-1 is as follows:

[0028] 1) Compounds 9 and 10 were condensed in acetonitrile at 50°C for 4 hours under the catalysis of 1-ethyl-(3-dimethylaminopropyl)carbodiimide, filtered, and concentrated to synthesize compounds 11.

[0029]

[0030] 2) Compound 11 and Compound 12 were reacted in N,N-dimethylformamide as a solvent under the catalysis of cesium carbonate at 20°C for 2.5 hours, filtered and concentrated to obtain Compound 13. The proton nuclear magnetic resonance spectrum of compound 13 is: 1H NMR (400MHz, Chloroform-d) δ8.43(d, J=1.6Hz, 1H), 7.88(dd, J=7.5, 1.4Hz, 1H), 7.76–7....

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Abstract

The invention discloses a PET tracer agent of a targeted CBR receptor and a preparation method and application of the PET tracer agent, the PET tracer agent is 18F-SQKJ-1, the structure of the PET tracer agent is shown in the specification, the tracer agent can target the CB1 receptor, namely, the tracer agent has selectivity to the CB1 receptor and can be imaged on the CB1 receptor in a high-quality mode, and therefore the compound can serve as the specific PET tracer agent to be used in the aspect of PET iconography. The CB1 receptor is closely related to mental diseases. Therefore, the < 18 > F-PET tracer agent is expected to be applied to imaging aspects such as PET / CT or PET / MR and the like, and is used for diagnosing mental diseases.

Description

technical field [0001] The invention belongs to the technical field of radiopharmaceuticals and nuclear medicine, and in particular relates to a PET tracer targeting CBR receptors and its preparation method and application. Background technique [0002] Positron Emission Tomography (PET) is currently the only new imaging technique that can display biomolecular metabolism, receptors, and neurotransmitter activities in vivo. It has been widely used in the diagnosis and differential diagnosis of various diseases, Efficacy evaluation, organ function research and new drug development, etc. PET imaging technology has high sensitivity, high specificity, and strong penetrability, and it can be used for whole-body imaging, and images of various regions of the whole body can be obtained in a one-time whole-body imaging examination. PET is an imaging that reflects molecular metabolism. When the disease is in the stage of molecular level changes in the early stage, the morphology and s...

Claims

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Application Information

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IPC IPC(8): C07D213/64A61K51/04A61K101/02
CPCC07D213/64A61K51/0455
Inventor 和庆钢何万里徐洋洋余开武靳晨阳李晓明张宏
Owner ZHEJIANG UNIV
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