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제108회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Gd Complexes of Macrocyclic Diethylenetriaminepentaacetic Acid (DTPA) Biphenyl-2,2`-bisamides as Strong Blood-Pool Magnetic Resonance Imaging Contrast Agents[Ⅲ-미발표]

등록일
2011년 8월 1일 14시 27분 47초
접수번호
1118
발표코드
Ⅲ-MEDI.P-321 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
금 <발표Ⅲ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
정기혜, 강민경1, 김태정
경북대학교 응용화학과, Korea
1경북대학교 의용생체공학과, Korea
We report the synthesis of macrocyclic DTPA conjugates of 2,2`-diaminobiphenyl and their Gd complexes of the type [Gd(L)(H2O)] 3 xH2O(2a,b; L = 1a,b) for use as new MRI blood-pool contrast agents (MRI BPCAs). Pharmacokinetic inertness of 2 compares well with those of analogous Gd-DTPA MRI CAs currently in use. The present system also shows very high stability in human serum. The R1 relaxivity reaches 10.9 mM-1 s-1, which is approximately 3 times as high as that of structurally related Gd-DOTA (R1 = 3.7mM-1 s1). The R1 relaxivity inHSA goes up to 37.2mM-1 s1, which is almost twice as high as that of MS-325, a leading BPCA, demonstrating a strong blood pool effect. The in vivo MR images of mice obtained with 2b are coherent, showing strong signal enhancement in heart, abdominal aorta, and small vessels. Even the brain tumor is vividly enhanced for an extended period of time. The structural uniqueness of 2 is that it is neutral in charge and thus makes no resort to electrostatic interaction, supposedly one of the essential factors for the blood-pool effect.

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