Hee-Kyung Kim1, Ki-Hye Jung2,
Min-Kyoung Kang1, Ji-Ae Park3, Seung-Tae Woo4,
Joo-Hyun Kim4, Tae-Jeong Kim2, Yongmin Chang1,5
1Department of Medical
& Biological Engineering, Kyungpook National University, Daegu, Korea,
Republic of; 2Department of Applied Chemistry, Kyungpook National
University, Daegu, Korea, Republic of; 3Laboratory of Nuclear
Medicine Research, Molecular Imaging Center, Korea Institute of Radiological
& Medical Science, Seoul, Korea, Republic of; 4Bayer Schering
Pharma Korea, Seoul, Korea, Republic of; 5Department of Diagnostic
Radiology & Molecular Medicine, Kyungpook National University, Daegu,
Korea, Republic of
Gd-complexes of the type [Gd(L)(H2O)]H2O(5a-c), where L is DOTA conjugates of tranexamic acid (4a)and tranexamic esters (4b-c), have been prepared as a new class of MRI BPCAs. Thermodynamic stability (KGdL) and pharmacokinetic inertness of 5 are compared well with or better than those of analogous MRI CAs such as Gd-DOTA and Gd-DTPA-BMA. Their R1-relaxivities are significantly higher than any of the clinically used MRI CAs. T1-weighted MR images of mice administered by 5c demonstrate high blood-pool effect with simultaneous contrast enhancement in liver.