Abstract #1681

Gd-Complexes of DOTA Conjugates of Tranexamates: A New Class of Non-Aromatic, Non-Ionic MRI Blood-Pool Contrast Agents

Hee-Kyung Kim¹, Ki-Hye Jung², Min-Kyoung Kang¹, Ji-Ae Park³, Seung-Tae Woo⁴, Joo-Hyun Kim⁴, Tae-Jeong Kim², Yongmin Chang^1,5

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 (K_GdL) 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.