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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 1
BKCSDE 35(1)
January 20, 2014 

Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-1,4,7-trisacetic Acid (DO3A) Conjugate of Tranexamates: A Quest for a Liver-specific Magnetic Resonance Imaging Contrast Agent
Ki-Soo Nam, Hyun-Jeong Jeong, Hee-Kyung Kim, Garam Choi, Kyung-Jin Suh, Yongmin Chang*, Tae-Jeong Kim*
MRI, Liver-specific contrast agents, Gadolinium, DO3A, Tranexamate
The work is directed toward the synthesis of a series of DO3A conjugates of tranexamates (1c-e) and their Gd complexes (2c-e) for use as a liver-specific MRI CA. All these complexes show thermodynamic and kinetic stabilities comparable to those of structurally related clinical agents such as Dotarem®. Their R1 relaxivities also compare well with those of commercial agent, ranging 3.68-4.84 mM1s1. In vivo MR images of mice with 2ae reveal that only 2a exhibits liver-specificity. Although 2b and 2c show strong enhancement in liver, yet no bile-excretion is observed to be termed as a liver-specific agent. The rest behaves much like ordinary ECF CAs like Dotarem®. The new series possess no toxicity to be employed in vivo.
87 - 92
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