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Imino acid PET imaging agent, and preparation method and application thereof

A PET imaging agent, imino acid technology, applied in organic chemistry methods, cyanide reaction preparation, chemical instruments and methods, etc., can solve the problems of complex metabolic mechanism and difficult in vivo quantitative research.

Active Publication Date: 2013-10-02
GUANGDONG HUIXUAN PHARMA TECH
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Problems solved by technology

A series of PET imaging agents reflecting amino acid transport have been developed rapidly, such as the widely used 11 C-labeled natural amino acid metabolism PET imaging agent (S- 11 C-methyl)-L-methionine ( 11 C-MET), but due to 11 C-MET is also involved in protein synthesis in a small amount, and inflammatory tissues will also have a high uptake of it, so the specificity needs to be improved; and 11 The metabolic mechanism of C-MET in vivo is relatively complex, and it is difficult to conduct quantitative research on it in vivo

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  • Imino acid PET imaging agent, and preparation method and application thereof
  • Imino acid PET imaging agent, and preparation method and application thereof
  • Imino acid PET imaging agent, and preparation method and application thereof

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Embodiment Construction

[0018] The present invention will be described in detail below in conjunction with specific embodiments.

[0019] 1. Materials and methods

[0020] 1.1 Instruments, reagents and experimental animals

[0021] Fluorine multifunctional chemical synthesis module PET-MF-2V-IT-I and carbon multifunctional module (Beijing Petrobio Co., Ltd., China); Agilent 1200 analytical HPLC analyzer (Agilent, USA); trifluoroform Silver sulfonyl (ACROS company, the United States); ethyl 2-bromopropionate, bis(p-nitrophenyl) carbonate, silver wire and graphite powder: 80 (Aldrich, the United States); phosphorus pentoxide (Beijing Chemical Reagent ); high performance liquid chromatography radioactive detector (Bioscan, USA); Cyclone10 / 5 cyclotron (IBA, Belgium); PET / CT () MicroPET (Siemens, Germany). Sep Pak QMA, Sep Pak HLB, Sep Pak C18 (Water, USA). PET-CT Gemini GXL scanner (Philips, Holland).

[0022] All experimental animals and cells were from the Animal Center of Sun Yat-Sen University, a...

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Abstract

The invention discloses an amino acid positron emission tomography (PET) imaging agent, and a preparation method and application thereof. The imaging agent belongs to the field of N-substituted positron nuclide labeled glutamic acid compound and has a structure as shown in the specification; and the L*represents -11CH3, CH2CH218F, and -COCH (18F) CH3. The novel imaging agent N-(2-18F-fluoropropionyl)-glutamic acid shows good tumor PET imaging sensitivity and specificity, has high uptake on tumor (such as S180 fibrosarcoma), and no obvious uptake on other tissues and organs (except for bladder) in the body, and indicates high tumor to background ratio. In vitro-in vivo experiments show that N-(2 - 18F -fluoropropionyl)-glutamic acid is stable in vitro and in vivo and shows good pharmacokinetic properties.

Description

technical field [0001] The present invention relates to imino acid positron emission tomography (PET) imaging agent and its preparation method and application, especially N-(2- 18 F-fluoropropionyl)-glutamic acid and N- 11 A preparation method of C-methyl-glutamic acid and its application to tumor PET imaging. Background technique [0002] 18 F-fluorodeoxyglucose ( 18 F-FDG) is currently the most commonly used glucose-metabolizing PET imaging agent. It has been successfully used in various clinical aspects, such as the identification of benign and malignant tumors, the evaluation of the malignant degree of tumors, and the monitoring of tumor treatment effects. but 18 F-FDG also has problems such as poor specificity, some tumor cells do not take it up, and inflammatory cells also take it up, which leads to certain false positive or false negative results in the differential diagnosis of tumors. The growth of tumor cells not only requires a large amount of glucose intake,...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/24C07C227/18C07B59/00A61K51/04A61K101/00A61K101/02
Inventor 唐刚华胡孔珍唐小兰王明芳黄文涛
Owner GUANGDONG HUIXUAN PHARMA TECH
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