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Preparation of technetium-99m tricarbonyl labeled glycine monomer or oligomer containing probes that have biomolecules and its application as imaging complex-composition

A technology of glycine trimer and glycine pentamer, applied in the preparation of organic compounds, peptide preparation methods, cyanide reaction preparation, etc., can solve the problems of reduced synthesis yield, reduced detection sensitivity, and reduced signal-to-noise ratio

Inactive Publication Date: 2014-12-31
KOREA ATOMIC ENERGY RES INST
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition to these two steps, other steps such as purification may be required, which leads to a decrease in the yield of the synthesis
[0006] When the radioligand used for imaging is not secreted from the body, non-specific signals are generated in vivo, which leads to a decrease in the signal-to-noise ratio and thus reduces detection sensitivity
In addition, radioactive ligands retained in the body increase the risk of overexposing the body to radiation

Method used

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  • Preparation of technetium-99m tricarbonyl labeled glycine monomer or oligomer containing probes that have biomolecules and its application as imaging complex-composition
  • Preparation of technetium-99m tricarbonyl labeled glycine monomer or oligomer containing probes that have biomolecules and its application as imaging complex-composition
  • Preparation of technetium-99m tricarbonyl labeled glycine monomer or oligomer containing probes that have biomolecules and its application as imaging complex-composition

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preparation example Construction

[0020] In addition, the present invention proposes a method for preparing technetium-99m-labeled glycine monomers or oligomers, including:

[0021] a) synthesis of technetium-99m tricarbonyl precursor; and

[0022] b) Labeling of glycine monomers or oligomers with technetium-99m tricarbonyl precursor.

preparation Embodiment 1

[0032] Preparation of technetium-99m-labeled glycine

[0033] Technetium-99m-labeled glycine monomers or oligomers according to the invention were prepared from the following materials.

[0034] ① Materials: Carbon monoxide was provided by Daehan Gas (Seoul, South Korea) and purified using an oxygen trap (trap) before use. Technetium-99m in the form of pertechnetate was prepared in 0.9% sodium chloride using a Unitech Tc-99m generator (Samyoung Unitech. Co., Ltd., Korea). Glycine, Gly-Gly-Gly (glycine trimer) and Gly-Gly-Gly-Gly-Gly (glycine pentamer) were purchased from Sigma Chemical Company (St. Louis, USA).

[0035] ② Animal test: Female sterile ICR mice (7 weeks old) were purchased from Orient Company (Seoul, South Korea) and domesticated for one week before using in the experiment. Mice were maintained in an environment with a relative humidity of 50 ± 5%, a temperature of 23 ± 2 °C, a 12-h light-dark cycle, allowed free access to food and water, and were acclimatized ...

Embodiment 1

[0037] Preparation of Technetium-99m Tricarbonylglycine Complex

[0038] Technetium-99m tricarbonyl precursor was applied to glycine monomers and oligomers to obtain technetium-99m tricarbonyl glycine.

[0039] Synthesis of Technetium-99m Tricarbonyl Precursor

[0040] by adding 1ml to a 5ml bottle of a commercially available generator 99m TCO 4 - (10mCi) preparation [ 99m Tc(CO) 3 (H 2 O) 3 ] + , containing borane potassium carbonate (potassium boranocarbonates) (5.9mg), sodium tetraborate decahydrate (2.85mg), dehydrated sodium tartrate (8.5mg) and sodium carbonate (7.15mg) in the 5ml bottle, and the solution was under nitrogen condition Heat in boiling water for 30 minutes. The labeling rate and stability of technetium-99m tricarbonyl precursor were detected by reversed-phase high-performance liquid chromatography.

[0041] For HPLC, an Agilent 1200 series (Agilent Technologies, Waldbronn, Germany) equipped with a vacuum degasser, binary pump, temperature-control...

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Abstract

Disclosed is a technetium-99m-labeled glycine oligomer associated with imaging probes for biomolecules of interest. The glycine oligomer can be readily synthesized in a single process using an automated peptide synthesizer. The technetium-99m tricarbonyl-labeled glycine oligomers can be useful as a radiotracer for gamma or SPECT imaging apparatus. The technetium-99m tricarbonyl-labeled glycine oligomers can be applied to various peptidyl biomolecules such as RGD peptide, somatostatin, neurotensin, etc., and exhibit rapid renal clearance without being excessively retained within the body.

Description

technical field [0001] The present invention relates to a method for preparing technetium-99m tricarbonyl-labeled glycine monomers or oligomers in a single process using automated peptide synthesis, and an imaging contrast combination containing technetium-99m tricarbonyl-labeled glycine monomers or oligomers thing. Background technique [0002] In an era where ideal tumor regulation is one of the main goals of modern medicine, scintillation detection and therapeutic techniques that enable the non-invasive observation of tumor status at the molecular level, using radiotracers that specifically react with target molecules, occupy a very important place , as it allows for early diagnosis and treatment of tumors. For example,[ 18 F]-FDG has been widely used as a radiopharmaceutical for positron emission tomography (PET) in tumor diagnosis, which provides information on angiogenesis and tumor metastasis. However, it has the disadvantage of not being able to diagnose brain tum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/04A61K49/12A61K49/08
CPCA61K51/025A61K51/0406A61K51/088A61K49/04A61K49/08A61K49/12A61K51/082A61K51/085C07B59/001C07B2200/05C07C227/16C07K1/13C07K5/0806C07K7/06
Inventor 张范洙朴相炫李柱相卢锺国
Owner KOREA ATOMIC ENERGY RES INST
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