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Gadolinium-based T1 magnetic resonance contrast agent FD-Gd-123 as well as preparation method and application thereof

A magnetic resonance contrast agent, fd-gd-123 technology, which is applied in the field of gadolinium-based T1 magnetic resonance contrast agent and magnetic resonance imaging angiography, and can solve the problem of low relaxation rate, high use dose, and superposition of safety risks of ionic chelate compounds. and other issues to achieve the effect of improving biosecurity

Pending Publication Date: 2022-03-15
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it has excellent structural stability, its relaxation rate is low and the dosage is high, which will bring the safety risks of free gadolinium ion toxicity and ionic chelate compound

Method used

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  • Gadolinium-based T1 magnetic resonance contrast agent FD-Gd-123 as well as preparation method and application thereof
  • Gadolinium-based T1 magnetic resonance contrast agent FD-Gd-123 as well as preparation method and application thereof
  • Gadolinium-based T1 magnetic resonance contrast agent FD-Gd-123 as well as preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0053]

[0054] Gd(NO 3 ) 3 6H 2 O (0.082g) and DO3A-S-pyridine-o-carboxylic acid (0.10g) were dissolved in 4ml methanol at a feed ratio of 1:1.1, and stirred. Adjust the pH to about 6 with 1M sodium hydroxide solution, react at room temperature for 0.5 h, and let stand overnight. After passing through a C-18 silica gel column and eluted with a gradient of 1% methanol / water, 0.06 g of white solid Gd-DO3A-S-pyridine-o-carboxylic acid I-S-1 was obtained. MS (ESI + ):m / z740.0011([M+Na] + ).

Embodiment 2

[0056]

[0057] Gd(NO 3 ) 3 6H 2 O (0.075g) and DO3A-S-pyridine p-carboxylic acid (0.10g) were dissolved in 18ml of water at a feed ratio of 1:1.2, and stirred. Adjust the pH to about 6 with 1M sodium hydroxide solution, react at 120°C for 24 h, and let stand overnight. C-18 silica gel column, 1% methanol / water gradient elution to obtain Gd-DO3A-S-pyridine p-carboxylic acid I-S-3 white solid 0.05g. MS (ESI + ):m / z655.0812([M+H] + ).

Embodiment 3

[0059]

[0060] Gd(AcO) 3 6H 2 O (0.041g) and DO3A-O-pyridine meta-carboxylic acid (0.05g) were dissolved in 2ml of water at a feed ratio of 1:1.1, and stirred. Adjust the pH to about 6 with 1M sodium hydroxide solution, react at room temperature for 24 hours, and let stand overnight. After passing through a C-18 silica gel column and eluted with a gradient of 1% methanol / water, 0.04 g of white solid Gd-DO3A-O-pyridine meta-carboxylic acid I-O-2 was obtained. MS (ESI + ):m / z639.1011([M+H] + ).

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Abstract

The invention relates to a gadolinium-based T1 magnetic resonance contrast agent FD-Gd-123 based on a pyridine carboxylate-triacetic acid-tetraazacyclododecane ligand, the general formula of the molecular structure of the gadolinium-based T1 magnetic resonance contrast agent FD-Gd-123 contains a pyridine carboxylate-triacetic acid-tetraazacyclododecane ligand (DO3A-PA), a nine-coordinated trivalent gadolinium (Gd) ion and n coordinated water molecules, and DO3A-PA is one of the two sites of pyridine carboxylate and 1, 4, 5, 6-tetraazacyclododecane ligand through an X group. The invention relates to a macrocyclic ligand which is formed by connecting 1, 4, 7-triacetic acid-1, 4, 7, 10-tetraazacyclododecane (DO3A) through a covalent bond. The contrast agent FD-Gd-123 disclosed by the invention not only has the advantages of a macrocyclic nonionic contrast agent Gd-DO3A and a macrocyclic high-stability contrast agent Gd-DOTA in structural design, but also has a T1 weighted magnetic resonance imaging value which is obviously higher than that of clinically used Gd-DOTA (3.6 mM <-1 > s <-1 >).

Description

technical field [0001] The invention relates to the field of magnetic resonance contrast agents, in particular to gadolinium T based on carboxylic acid pyridine-triacetic acid-tetraazacyclododecane ligands 1 Magnetic resonance contrast agent FD-Gd-123 and its preparation method and application of magnetic resonance imaging contrast. Background technique [0002] Magnetic resonance imaging (MRI) has attracted widespread attention due to its high spatial resolution, non-invasiveness, and good imaging effect on soft tissues, and has become one of the indispensable clinical diagnostic techniques. In order to improve the clarity of imaging, improve the accuracy of diagnosis, and expand the range of imaging tissues, the development of magnetic resonance contrast agents with high relaxation rates has received extensive attention (Chem. Rev. 2019, 119, 957-1057). The MRI contrast agents used in clinical practice are mainly gadolinium-based contrast agents. The trivalent gadolinium...

Claims

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Application Information

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IPC IPC(8): C07F3/08A61K49/10
CPCC07F3/08A61K49/108
Inventor 凌云周亚明杨永泰刘小锋贾瑜尹波耿永印
Owner FUDAN UNIV
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