Ogan M D, Schmiedl U, Moseley M E, Grodd W, Paajanen H, Brasch R C
Department of Radiology, University of California, San Francisco.
Invest Radiol. 1987 Aug;22(8):665-71.
A paramagnetic-labeled macromolecule, albumin-(Gd-DTPA), was prepared for use as an intravascular contrast agent for magnetic resonance imaging. An average of 19 Gd-DTPA chelates were covalently conjugated to human serum albumin through the bifunctional anhydride of DTPA. The albumin-(Gd-DTPA) was characterized with use of high-performance liquid chromatography, sodium dodecyl sulfate gel electrophoresis, atomic absorption, biuret and Bradford protein tests, and by its effect on proton relaxation (relaxivity). The average molecular weight was 92,000 daltons, indicating the albumin conjugate was predominantly monomeric. The T1 relaxivity of albumin-(Gd-DTPA) was 273 mM-1 sec-1 relative to carrier concentration, which corresponds to a relaxivity of 14.9 mM-1 sec-1 relative to gadolinium concentration. The average conditional stability constant for albumin-bound Gd-DTPA chelate was log K = 20.0. Spin-echo images of rats demonstrated persistent enhancement of vascular tissues and slowly flowing blood. Application of albumin-(Gd-DTPA) may augment the MR assessments of blood volume, tissue perfusion, and flow characteristics.
制备了一种顺磁性标记的大分子,即白蛋白 -(钆 - 二乙三胺五乙酸),用作磁共振成像的血管内造影剂。平均19个钆 - 二乙三胺五乙酸螯合物通过二乙三胺五乙酸的双功能酸酐与人类血清白蛋白共价结合。使用高效液相色谱、十二烷基硫酸钠凝胶电泳、原子吸收、双缩脲和考马斯亮蓝蛋白检测以及其对质子弛豫(弛豫率)的影响对白蛋白 -(钆 - 二乙三胺五乙酸)进行了表征。平均分子量为92,000道尔顿,表明白蛋白缀合物主要是单体。相对于载体浓度,白蛋白 -(钆 - 二乙三胺五乙酸)的T1弛豫率为273 mM-1 sec-1,相对于钆浓度相当于14.9 mM-1 sec-1的弛豫率。白蛋白结合的钆 - 二乙三胺五乙酸螯合物的平均条件稳定常数为log K = 20.0。大鼠的自旋回波图像显示血管组织和缓慢流动的血液持续增强。白蛋白 -(钆 - 二乙三胺五乙酸)的应用可能会增强对血容量、组织灌注和血流特性的磁共振评估。