Unit of Academic Radiology, Royal Hallamshire Hospital, University of Sheffield, Sheffield, UK.
Contrast Media Mol Imaging. 2010 Jan-Feb;5(1):39-43. doi: 10.1002/cmmi.366.
A new contrast agent was developed by linking Gd-DTPA chelate to recombinant human albumin in the laboratory. The molar relaxivity of the new agent was tested in aqueous solution at B(0) 1.5 T and temperature 20 degrees C. The soluble compound had a higher molar longitudinal relaxivity and molar transverse relaxivity in water (r(1) = 7.2 s(-1) mM(-1), r(2) = 18.4 s(-1) mM(-1)) than those measured for Gd-DTPA solution (r(1) = 3.5 s(-1) mM(-1), r(2) = 5.5 s(-1) mM(-1)). The performance of the compound as a blood pool agent was investigated with soluble and microparticulate forms of the compound and comparisons were made with Gd-DTPA and the polymeric blood-pool agent, Gadomer. T(1)-weighted imaging experiments show that the soluble compound acts as a highly effective blood pool agent with hyperintensity in the vasculature persisting beyond 2 h post administration, compared with free Gd-DTPA, which was cleared from the blood pool after approximately 10 min. The clearance kinetics of the new agents were examined, due to the incomplete elimination within 14 days post injection; both rHA labeled compounds are probably not suitable for development as routine blood pool contrast media. However, with free sites on the Gd-loaded rHA molecule, there are possibilities for binding the agent to antibodies in the laboratory, which was demonstrated, and thus there exist potential applications for in vivo molecular imaging with this agent.
实验室中将 Gd-DTPA 螯合物与重组人血清白蛋白相连接,开发出一种新型的对比剂。在 B(0)为 1.5T 和温度为 20 摄氏度的水溶液中测试了新型试剂的摩尔弛豫率。该可溶性化合物在水中具有更高的摩尔纵向弛豫率和摩尔横向弛豫率(r1=7.2 s-1mM-1,r2=18.4 s-1mM-1),高于 Gd-DTPA 溶液的测量值(r1=3.5 s-1mM-1,r2=5.5 s-1mM-1)。通过可溶性和微粒形式的化合物研究了该化合物作为血池试剂的性能,并与 Gd-DTPA 和聚合血池试剂 Gadomer 进行了比较。T1 加权成像实验表明,与自由 Gd-DTPA 相比,可溶性化合物在给药后 2 小时以上的血管中具有高强度的超顺磁性,作为一种非常有效的血池试剂。由于在注射后 14 天内不完全清除,新试剂的清除动力学得到了检查;由于 rHA 标记的两种化合物在注射后 14 天内不能完全清除,因此都不太可能开发为常规血池造影剂。然而,由于 Gd 负载的 rHA 分子上有游离的位点,因此有可能在实验室中将该试剂与抗体结合,这已经得到了证明,因此该试剂可能存在用于体内分子成像的潜在应用。