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Developer for PET/CT (positron emission tomography/computer tomography)

An imaging agent and developer technology, applied in the preparation of organic compounds, chemical instruments and methods, organic chemistry, etc., can solve problems such as false positives, achieve good targeting, good safety and stability, and imaging long-lasting effect

Active Publication Date: 2016-01-06
GUANGDONG PHARMA UNIV
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  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] but 18 F-FDG is a non-tumor-specific tracer. In addition to the physiological uptake of normal tissues, some benign lesions such as inflammation, active tuberculosis, sarcoidosis, inflammatory pseudotumor, and post-radiotherapy and post-operative reactions can all be manifested as 18 High F-FDG uptake, leading to false positive results

Method used

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  • Developer for PET/CT (positron emission tomography/computer tomography)
  • Developer for PET/CT (positron emission tomography/computer tomography)
  • Developer for PET/CT (positron emission tomography/computer tomography)

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Embodiment Construction

[0022] English abbreviations are as follows:

[0023] 18 F-NFP is 4-nitrobenzene-2- 18 F-propionate, DMSO is dimethylsulfoxide, DIPEA is N,N-diisopropylethylamine, FP-Arg is N -(2-fluoropropionyl)- L -Arginine ， 18 F-FP-Arg is N- (2- 18 F-fluoropropionyl)- L - Arginine.

[0024] A kind of imaging agent for PET / CT, described imaging agent is N -(2- 18 F-fluoropropionyl)- L - Arginine.

[0025] A preparation method for a developer for PET / CT, comprising the following steps:

[0026] 1) Preparation 18 f - Ions: radionuclides produced by cyclotron nuclear reactions 18 f - Ions, captured by the QMA column 18 f - ions, then with K 222 solution pair 18 f - Ions were eluted, the excess solvent and water in the eluent were removed, and nitrogen was blown to dry to obtain dry 18 f - ion.

[0027] 2) Under the condition of heating at 100°C for 10 minutes, the 18 f - The ions were reacted with ethyl 2-bromopropionate, potassium hydroxide, and bis(p-nitrophenyl)ca...

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Abstract

The invention discloses a developer for PET / CT (positron emission tomography / computer tomography). The developer is N-(2-<18>F-fluoro propionyl)-L-arginine, and auxiliary radicals, namely 4-nitrobenzene-2-<18>F-propionate and L-arginine ethyl ester dihydrochloride, carry out amiation reaction and are further hydrolyzed to obtain the developer. The developer has the advantages that the developer is better in targeting for lung cancers in human lung cancer bearing nude mouse models and is lower in brain-muscle extraction ratio and excellent in safety and stability; development effects of the developer are superior to development effects of <18>F-FDG (fluorodeoxyglucose), and the developer is long in development hold time; the <18>F-FP-Arg developer can possibly become an excellent lung cancer developer and a developer for various other cancers except for cancers of livers and kidneys in the future.

Description

technical field [0001] The present invention relates to an imaging agent for PET / CT. Background technique [0002] Molecular imaging plays a huge role in tumor diagnosis, and positron emission computed tomography (PET / CT), which has emerged in recent years, is an important part of it. PET / CT has obvious advantages in tumor staging and typing, identification of benign and malignant tumors, and evaluation of curative effect. With the help of PET drugs, dynamic biological information about the energy metabolism of tumor tissues that cannot be given by CT or magnetic resonance imaging (MRI) can be provided. [0003] Currently widely used imaging agents are 18 F-fluorodeoxyglucose ( 18 F-fluorodeoxyglucose, 18 F-FDG), which enjoys the name of century molecular 18 F-FDG is currently the most widely used positron imaging agent. Glucose is an important energy substrate for the human body, and the glucose metabolism of tissues and organs reflects their functional status to a la...

Claims

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Application Information

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IPC IPC(8): A61K51/04C07C277/08C07C279/14A61K101/02
Inventor 臧林泉高思远
Owner GUANGDONG PHARMA UNIV
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