Yu Kai-chao, Liu Liu-yi, Wan Fu-xian, Zhou Jin-lan, Ding Shang-wu, Ye Chao-hui
Department of Chemistry, Huazhong University of Science and Technology, Wuhan, China.
Guang Pu Xue Yu Guang Pu Fen Xi. 2006 Apr;26(4):670-3.
To look for new MRI (magnetic resonance imaging) contrast agents with higher relaxivity as well as liver-selecsivity, four novel ester-amino ligands were synthesized by bis-acylation of octadecanyl, hexadecanyl, tetradecanyl and dedecanyl L-lysine with diethylenetriaminepentaacetic acid mono-anhydride (DTPA-MA), respectively. The corresponding dimeric Gd(III) complexes were gained by the reaction of these ligands with GdCl3 x 6H2O. All ligands and complexes were characterized by FTIR, 1H NMR and elemental analysis. The longitudinal relaxation time (T1) was measured, and relevant longitudinal relaxivity (R1) of these neatral binuclear Gd(III) complexes is: 6.48, 6.02, 5.76 and 5.68 L x mmol(-1) x s(-1), respectively, and all are higher than that of Gd-DTPA (4.98 L x mmol(-1) x s(-1)) (300 MHz).
为寻找具有更高弛豫率以及肝脏选择性的新型磁共振成像（MRI）造影剂，分别通过十八烷基、十六烷基、十四烷基和十二烷基L-赖氨酸与二乙烯三胺五乙酸单酐（DTPA-MA）的双酰化反应合成了四种新型酯-氨基配体。这些配体与GdCl₃·6H₂O反应得到相应的二聚体Gd(III)配合物。所有配体和配合物均通过傅里叶变换红外光谱（FTIR）、¹H核磁共振（¹H NMR）和元素分析进行了表征。测量了纵向弛豫时间（T1），这些中性双核Gd(III)配合物的相关纵向弛豫率（R1）分别为：6.48、6.02、5.76和5.68 L·mmol⁻¹·s⁻¹，且均高于Gd-DTPA（4.98 L·mmol⁻¹·s⁻¹）（300 MHz）。
