Synthesis Neutral Rare Earth Complexes of Diethylenetriamine-N,N"-bis(acetyl-isoniazid)-N,N',N"-triacetic Acid as Potential Contrast Enhancement Agents for Magnetic Resonance Imaging
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概要
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A novel ligand, diethylenetriamine-N,N"-bis(acetyl-isoniazid)-N,N',N"-triacetic acid (H_3L) has been synthesized from diethylene triamine pentaacetic acid (DTPA) and isoniazid. Ligand and its five neutral rare earth (RE=La, Sm, Eu, Gd, Tb) complexes holding promise of magnetic resonance imaging (MRI) were characterized on the basis of elemental analysis, molar conductivity, ^1H-NMR spectrum, FAB-MS, TG-DTA analysis and IR spectrum. The relaxivity (R_1) of complexes and Gd(DTPA)^<2-> used as a control were determined. The relaxivity of LaL, SmL, EuL, GdL, TbL and Gd(DTPA)^<2-> were 0.14, 1.66, 3.14, 6.08, 2.79 and 4.34 l・mmol^<-1>・s^<-1>, respectively. The spin-lattice relaxivity of GdL was larger than that of Gd(DTPA)^<2->. The relaxivity of GdL had also been investigated in human serum albumin (HSA) solution, the relaxivity of GdL was enhanced from 6.08 l・mmol^<-1> s^<-1> in water solution to 9.09 l・mmol^<-1>・s^<-1> in HSA solution. In addition, thermodynamics stability constant of GdL complex was determined, the thermodynamic stability constant of GdL complex (K_<GdL>=10^<20.84>) was a few larger than that of Gd(DTPA)^<2-> (K_<Gd-DTPA>=10^<20.73>). The results showed that complex of GdL may be a prospective MRI contrast agent with low osmotic pressure due to non-ion complex, high spin-lattice relaxivity, good stability and binding affinity for the serum protein.
- 2006-08-01
著者
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Zhang Shi-Ping
State Key Laboratory of Natural and Biomimetic Drugs, Peking University
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Zhang Shi-ping
State Key Laboratory Of Applied Organic Chemistry College Of Chemistry And Chemical Engineering Lanz
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ZHANG Ding-Wa
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering Lan
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YANG Zheng-Yin
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering Lan
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WANG Bao-Dui
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering Lan
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YANG Ru-Dong
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering Lan
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Yang Zheng-yin
Coll. Of Chemistry And Chemical Engineering And State Key Lab. Of Applied Organic Chemistry Lanzhou
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Wang Bao-dui
College Of Chemistry And Chemical Engineering And State Key Laboratory Of Applied Organic Chemistry
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Wang Bao-dui
Coll. Of Chemistry And Chemical Engineering And State Key Lab. Of Applied Organic Chemistry Lanzhou
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Zhang Ding-wa
State Key Laboratory Of Applied Organic Chemistry College Of Chemistry And Chemical Engineering Lanz
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Yang Ru-dong
State Key Laboratory Of Applied Organic Chemistry College Of Chemistry And Chemical Engineering Lanz
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Zhang Shi-ping
State Key Lab. Of Natural And Biomimetic Drugs Peking Univ.
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