Evaluation of rHA labeled with Gd-DTPA for blood pool imaging and targeted contrast delivery.
Evaluation of rHA labeled with Gd-DTPA for blood pool imaging and targeted contrast delivery.
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DOI：
10.1002/cmmi.366
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发表时间：
2010
影响因子：
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通讯作者：
J. Wild;J. Woodrow;E. V. van Beek;B. Misselwitz;R. Johnson
中科院分区：
文献类型：
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作者：
J. Wild;J. Woodrow;E. V. van Beek;B. Misselwitz;R. Johnson
在实验室将Gd-DTPA螯合物与重组人血白蛋白偶联，研制成一种新的造影剂。在B（0）1.5 T和温度20 ℃下在水溶液中测试新试剂的摩尔弛豫率。可溶性化合物在水中的摩尔纵向弛豫率和摩尔横向弛豫率（r（1）= 7.2 s（-1）mM（-1），r（2）= 18.4 s（-1）mM（-1））高于Gd-DTPA溶液的测量值（r（1）= 3.5 s（-1）mM（-1），r（2）= 5.5 s（-1）mM（-1））。用可溶性和微粒形式的化合物研究了化合物作为血池剂的性能，并与Gd-DTPA和聚合物血池剂Gadomer进行了比较。T（1）加权成像实验表明，与游离Gd-DTPA相比，可溶性化合物作为一种高效的血池剂，与游离Gd-DTPA相比，游离Gd-DTPA在约10分钟后从血池中清除，在给药后2小时内血管系统中持续高强度。由于注射后14天内不完全消除，因此检查了新药物的清除动力学;两种rHA标记的化合物可能都不适合作为常规血池造影剂开发。然而，由于Gd负载的rHA分子上有游离位点，因此有可能在实验室中将该试剂与抗体结合，这已得到证实，因此该试剂在体内分子成像中存在潜在应用。
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.