title: Gd Complexes of DO3A-(Biphenyl-2,2'-bisamides) Conjugates as MRI Blood-Pool Contrast Agents.
abstract: We report the synthesis of DO3A derivatives of 2,2'-diaminobiphenyl (1a,b) and their Gd complexes of the type [Gd(1)(H2O)]·xH2O (2a,b) for use as new MRI blood-pool contrast agents (BPCAs) 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. The R 1 relaxivity in water reaches 7.3 mM(-1) s(-1), which is approximately twice as high as that of Dotarem (R 1 = 3.9 mM(-1) s(-1)). They show interaction with HSA to give association constants (K a) in the order of two (∼10(2)), 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. Furthermore, the brain tumor is vividly enhanced for an extended period of time.
authors.affiliation: Department of Applied Chemistry, Department of Medical & Biological Engineering, and Department of Chemistry, Kyungpook National University , University Road 80, Daegu, 702-701, Korea.
authors.forename: Ki-Hye
authors.initials: KH
authors.lastname: Jung
authors.affiliation: Department of Applied Chemistry, Department of Medical & Biological Engineering, and Department of Chemistry, Kyungpook National University , University Road 80, Daegu, 702-701, Korea.
authors.forename: Hee-Kyung
authors.initials: HK
authors.lastname: Kim
authors.affiliation: Molecular Imaging Research Center, Korea Institute of Radiological Medical Science , Nowon-gil 75, Seoul, 139-706, Korea.
authors.forename: Ji-Ae
authors.initials: JA
authors.lastname: Park
authors.affiliation: Department of Applied Chemistry, Department of Medical & Biological Engineering, and Department of Chemistry, Kyungpook National University , University Road 80, Daegu, 702-701, Korea.
authors.forename: Ki Soo
authors.initials: KS
authors.lastname: Nam
authors.affiliation: Department of Applied Chemistry, Department of Medical & Biological Engineering, and Department of Chemistry, Kyungpook National University , University Road 80, Daegu, 702-701, Korea.
authors.forename: Gang Ho
authors.initials: GH
authors.lastname: Lee
authors.affiliation: Department of Applied Chemistry, Department of Medical & Biological Engineering, and Department of Chemistry, Kyungpook National University , University Road 80, Daegu, 702-701, Korea ; Department of Radiology & Molecular Medicine, Kyungpook National University , Dongin-dong 2-ga, Daegu, 700-422, Korea.
authors.forename: Yongmin
authors.initials: Y
authors.lastname: Chang
authors.affiliation: Department of Applied Chemistry, Department of Medical & Biological Engineering, and Department of Chemistry, Kyungpook National University , University Road 80, Daegu, 702-701, Korea.
authors.forename: Tae-Jeong
authors.initials: TJ
authors.lastname: Kim
keywords: DO3A; Gd chelates; MRI BPCA; biphenyl; brain tumor