Ki-Hye Jung1, Hee-Kyung Kim2, Min-Kyoung Kang2, Ji-Ae Park3, Eun-Young Jeon4, Seung-Tae Woo5, Joo-Hyun Kim5, Tae-Jeong Kim1, Yongmin Chang2, 6
1Applied Chemistry, Kyungpook National University, Daegu, Korea; 2Medical & Biological Engineering, Kyungpook National University, Daegu, Korea; 3Molecular Imaging Research Center, Korea Institute of Radiological & Medical Science, Seoul, Korea; 4The Advanced Medical Technology Cluster for Diagnosis & Prediction, Kyounpook National University, Daegu, Korea; 5Bayer Healthcare, Medical care, Seoul, Korea; 6Diagnostic Radiology and Molecular Medicine, Kyungpook National University, Daegu, Korea
We report the synthesis of DO3A derivatives of 2,2&[prime]- diaminobiphenyl and their Gd complexes of the type [Gd(1)(H2O)]&[middot] xH2O (2a, b)for use as new MRI blood-pool contrast agents that provide strong and prolonged vascular enhancement. Pharmacokinetic inertness of 2 compares well with that of structurally related Dotarem, a DOTA-based MRI CA currently in use. They show interaction with HSA to give association constants (Ka) in the order of two (102), revealing the existence of the blood-pool effect. The in-vivo MR images of mice obtained with 2 are coherent, showing strong signal enhancement in both heart, abdominal aorta, and small vessels.