Li Cong, Li Ying-Xia, Law Ga-Lai, Man Kwan, Wong Wing-Tak, Lei Hao
Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong, PR China.
Bioconjug Chem. 2006 May-Jun;17(3):571-4. doi: 10.1021/bc060003m.
A bis-hydrated Gd3+ complex based on tris acetic acid-1,4,7,10-tetraazacyclododecane (DO3A) that was functionalized with aza-15-crown-5 demonstrated a nearly optimal water-exchanging rate (k(ex) = 3.1 x 10(7) s(-1)) and low acute cytotoxicity. Efficient magnetic resonance signal intensity enhancements and prolonged residence lifetime induced by this small molecular complex in vivo were demonstrated even with one-fifth of the standard dosage used in the clinic.
一种基于三乙酸-1,4,7,10-四氮杂环十二烷(DO3A)并经氮杂-15-冠-5官能化的双水合钆(Gd3+)配合物表现出近乎最佳的水交换速率(k(ex) = 3.1 x 10(7) s(-1))且急性细胞毒性较低。即便使用临床标准剂量的五分之一,这种小分子配合物在体内也能实现高效的磁共振信号强度增强及延长的驻留寿命。