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Gd-Complexes of DTPA-bis(amide) Conjugates of Tranexamic Acid and Its Esters with High Relaxivity and Stability for Magnetic Resonance Imaging

등록일
2008년 2월 14일 10시 04분 57초
접수번호
1243
발표코드
28P162포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
금 <발표Ⅳ>
발표형식
포스터
발표분야
무기화학
저자 및
공동저자
김희경, 박지애, Pattubala A N Reddy1, 김태정1
경북대학교 의용생체공학과,
1경북대학교 응용화학과,
The synthesis and the characterization of a series of DTPA-bis(amides) conjugates of tranexamic acid (L1), its esters (L2-L6), and their Gd(III) complexes of the type [Gd(L)(H2O)]•nH2O (L = L1-L6) are described. Except for the case of L1, all Gd-complexes exhibit greatly enhanced R1 relaxivity. Highest R1 reaches up to 12.9 mM-1sec-1 for [Gd(L2)(H2O)]. Such high relaxivity is reflected in the intensity enhancement of the on H-ras transgenic mice bearing hepatic tumor in the in vivo MRI study. Thermodynamic stability constants, conditional stability constants, and the pM values demonstrate higher stability of [Gd(L)(H2O)]•nH2O (L = L1-L6) than Omniscan? under physiological conditions. The MTT assay performed on these complexes reveals cytotoxicity as low as that for Omniscan? in the concentration range required to obtain intensity enhancement in the in vivo MRI study.

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