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<99m>tco(MNXT)2 complex, as well as preparation method and application thereof

A technology of 99mtc and 99mtco, applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of high liver uptake and low tumor uptake

Inactive Publication Date: 2013-03-20
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

because 99m The TcN triple bond has high chemical stability and special biodistribution properties, and a kind of 99m TcN nuclear labeled metronidazole xanthate complex ( 99m TcN(MNXT) 2 ) as a potential tumor hypoxia imaging agent (Madhaba B. Mallia, Meera Venkatesh, et a1.A novel[ 99m TcN] 2+ complex of metronidazole xanthate as a potential agent for targeting hypoxia..Bioorganic&Medicinal Chemistry Letters, 2005, 15: 3398-3401), but its tumor uptake value is low and liver uptake value is high, so it is still necessary to develop a more ideal new tumor hypoxia imaging agent

Method used

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  • &lt;99m&gt;tco(MNXT)2 complex, as well as preparation method and application thereof
  • &lt;99m&gt;tco(MNXT)2 complex, as well as preparation method and application thereof
  • &lt;99m&gt;tco(MNXT)2 complex, as well as preparation method and application thereof

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Embodiment Construction

[0033] Describe the present invention in detail below by embodiment: a kind of 99m TcO(MNXT) 2 Compound, its structural formula is:

[0034]

[0035] In the structural formula: with [ 99m TcO] 3+ The core is the central core, and the four sulfur atoms in the two MNXT ligand molecules are 99m Tc coordinates to get 99m TcO(MNXT) 2 Complexes.

[0036] 99m TcO(MNXT) 2 The preparation method of the complex is as follows:

[0037] Preparation of GH freeze-dried kit: by mixing GH, SnCl 2 .2H 2 O is dissolved in an appropriate amount of secondary water according to the weight ratio of 200:1, and after fully dissolving, it is divided into clean penicillin vials, freeze-dried and set aside, and then the 74MBq 99m TCO 4 - Add 1-2mL of the eluent into the GH freeze-dried kit, shake well, and react at room temperature (20-30°C) for 15 minutes to obtain 99m Tc-GH solution; adjusted with 0.1mol / L NaOH 99m The pH value of the Tc-GH solution is 9-10, and 1 mL of MNXT aqueous ...

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Abstract

The invention discloses a <99m>TcO(MNXT)2 complex, as well as a preparation method and application thereof. According to the complex, <99m>TcO core is used as a central core, and 4 sulfur atoms of two MNXT ligand molecules are complexed with <99m>Tc to obtain the <99m>TcO(MNXT)2 complex. The <99m>TcO(MNXT)2 complex prepared by a ligand exchange method is good in hydrophilic property and high in tumor uptake, has certain hypoxic selectivity and high tumor / muscle and tumor / blood ratios, and can be prepared into a novel tumor hypoxic developing agent with excellent performance.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a 99m TcO(MNXT) 2 Compounds and their preparation methods and applications. Background technique [0002] Tissue hypoxia is the main feature of many clinically important diseases, and tissue hypoxia is common in human and animal tumors. Due to the existence of hypoxia, the tumor is resistant to radiotherapy and chemotherapy, making the tumor difficult to cure and easy to relapse. Detecting the oxygen level of the tumor before and after the treatment of tumor patients is of great significance for detecting malignant tumors and their metastases to judge the therapeutic effect. There are many methods for testing tumor hypoxia, among which radionuclide imaging in nuclear medicine is one of them. Link radionuclides to radiosensitizer molecules to form tumor hypoxia imaging drugs that specifically bind to hypoxic cells, and non-in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
Inventor 张俊波李贞翔陆洁罗超慧王学斌唐志刚
Owner BEIJING NORMAL UNIVERSITY