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Technetium carbonyl marked 2-nitroimidazole complex as well as preparation method and application thereof

A technology of nitroimidazole and carbonyl technetium, applied in the field of radionuclide-labeled compounds, can solve the problems of unsatisfactory clinical imaging performance, low absolute tumor uptake, slow tissue clearance, etc. Imaging diagnostic effect and drug intake improvement effect

Inactive Publication Date: 2010-12-22
LANZHOU UNIVERSITY
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  • Abstract
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  • Claims
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Problems solved by technology

[0004] Tumor hypoxia imaging agents that have been used in clinical research include 18 FMISO, 99m Tc-HL91, 64 Cu-ATSM, etc., but their clinical imaging performance is not ideal. The main problems include low absolute tumor uptake, slow clearance of normal tissues, radioactive concentration in the liver and abdomen, etc.
In order to obtain tumor hypoxia imaging agents with better imaging properties, researchers at home and abroad have conducted extensive and in-depth research and explored a series of 18 F. 99m Tc, 123 / 125 I and 62 / 64 Cu and other labeled nitroimidazole or non-nitroimidazole derivatives, but unfortunately there is no substantial breakthrough in clinical imaging value of these derivatives

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  • Technetium carbonyl marked 2-nitroimidazole complex as well as preparation method and application thereof
  • Technetium carbonyl marked 2-nitroimidazole complex as well as preparation method and application thereof
  • Technetium carbonyl marked 2-nitroimidazole complex as well as preparation method and application thereof

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preparation example Construction

[0058] Preparation method of carbonyl technetium-labeled 2-nitroimidazole complex

[0059] [ 99m Tc(CO) 3 (NNN-PEG 3 -NIM)] + , [ 99m Tc(CO) 3 (NNO-PEG 3 -NIM)] and [ 99m Tc(CO) 3 (NOO-PEG 3 -NIM)] - Preparation of:

[0060] Freshly prepared [ 99m Tc(CO) 3 (H 2 O) 3 ] + The intermediate was adjusted to pH = 7 with 1N and 0.01N hydrochloric acid; 0.1 mL of 500 μg / mL NNN-PEG was added to a vial 3 -NIM or NNO-PEG 3 -NIM or NOO-PEG 3 -NIM ligand solution, 0.4mL intermediate solution (10mCi) whose pH value has been adjusted and 0.5mL PBS solution with pH=7.4, shake well and heat in a boiling water bath for 15min to obtain the desired product. The structural formula of each corresponding product is shown in formula 3:

[0061]

[0062] [ 99m Tc(CO) 3 (NNN-PEG 3 -NIM)] + [ 99m Tc(CO) 3 (NNO-PEG 3 -NIM)] [ 99m Tc(CO) 3 (NOO-PEG 3 -NIM)] -

[0063]

[0064] Formula 3: Structure of carbonyl technetium-labeled 2-nitroimidazole complex

[0065] Detect...

Embodiment 4

[0068] Example 4: Lipid-water partition coefficient of carbonyl technetium-labeled 2-nitroimidazole complexes

[0069] Mix equal volumes of n-octanol and phosphate buffer (25mM, pH=7.4), add an appropriate amount of labeled complex to be tested, shake fully, and centrifuge at high speed to separate layers, take equal volumes of organic phase and aqueous phase, and measure the two phases respectively. The radioactive count of the phase, the partition coefficient P of the complex to be measured is the ratio of the radioactive count of the organic phase to the aqueous phase, and the operation is repeated many times to obtain the average value. The lipid-water partition coefficient is generally expressed in LogP.

[0070] Measurement result shows that each complex is water-soluble, [ 99m Tc(CO) 3 (NNN-PEG 3 -NIM)] + , [ 99m Tc(CO) 3 (NNO-PEG 3 -NIM)] and [ 99m Tc(CO) 3 (NOO-PEG 3 -NIM)] - The Log P values ​​were -1.11±0.08, -0.44±0.10, -1.64±0.10, respectively.

[0071...

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Abstract

The invention discloses a technetium carbonyl marked 2-nitroimidazole complex as well as a preparation method and application thereof, wherein the technetium carbonyl marked 2-nitroimidazole complex is a radionuclide-marked compound. The preparation method of the technetium carbonyl marked 2-nitroimidazole complex comprises the following steps of: firstly synthesizing ligands of NNN-PEGn-NIM or NNO-PEGn-NIM or NOO-PEGn-NIM, and then respectively heating each ligand and freshly prepared [<99m>Tc (CO) 3 (H2O) 3]<+> intermediate in boiling water bath and making the ligand and the freshly prepared [<99m>Tc (CO) 3 (H2O) 3]<+> intermediate react to obtain the corresponding technetium carbonyl marked 2-nitroimidazole complex. The technetium carbonyl marked 2-nitroimidazole complex is condensed in hypoxic tumor cells through the target action of nitroimidazole and can be used for SPECT (Single Photon Emission Computed Tomography) development diagnosis of the hypoxic tumor cells.

Description

technical field [0001] The present invention relates to a class of compounds labeled with radioactive nuclides, as well as the preparation method and application of the compounds. Specifically, the present invention relates to carbonyl technetium-labeled 2-nitroimidazole complexes. Background technique [0002] Malignant tumor is one of the main diseases that lead to abnormal death of human beings, and it ranks in the forefront of disease mortality and cause of death in my country and the world. Hypoxia is a common characteristic of human and animal tumors. Experimental observation and measurement show that the proportion of hypoxic cells in solid tumors is generally 10-20%, and some even reach 50%. At present, in addition to surgery, the treatment methods for malignant tumors are mainly radiotherapy and chemotherapy, but hypoxia makes the tumor tissue insensitive to radiotherapy and chemotherapy, which greatly improves its resistance to radiotherapy and chemotherapy; at the...

Claims

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Application Information

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IPC IPC(8): C07F13/00C07D233/91A61K51/04A61K103/10
Inventor 汪建军郑小北杨晶吴王锁
Owner LANZHOU UNIVERSITY
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