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用吡哆胺(PM)作为肝靶向基团,先与DTPA双N-羟基琥珀酰亚胺活性酯(SuO-DTPA-OSu)反应生成含一个吡哆胺的DTPA单N-羟基琥珀酰亚胺活性酯(SuO-DTPA-PM),再分别与α,β-聚(2-羟乙基)-L-天冬酰胺和α,β-聚(2-胺乙基)-L-天冬酰胺反应,合成了2类肝靶向性大分子配体,并制备了它们的Gd(Ⅲ)配合物.对所合成的大分子配体以及钆配合物进行了表征.测试了配合物的弛豫率.初步测试大分子载体PHEA和PAEA及其钆配合物的细胞毒性.研究了大分子配体在小白鼠体内分布和大分子钆配合物对大白鼠肝脏造影成像性能.结果表明,与临床广泛应用的小分子磁共振成像造影剂Gd-DTPA相比,以上2类大分子造影剂的弛豫率有明显的提高,并且具有较好的肝靶向性和肝脏成像对比度及清晰度. 相似文献
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用核磁共振成象方法研究了由印防已毒素(picrotoxin)诱发的大白鼠癫痫模型脑组织中水的双指数扩散现象.对模型诱发前后进行自身对照发现，在癫痫发作期间水扩散系数在全脑范围内特别在海马区和皮质区明显下降，同时快扩散部分的相对含量有所增加.本文根据核磁共振理论，对扩散系数的这种变化做了解释.此结果对于揭示癫痫发作的机制具有参考价值. 相似文献
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Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (DTPA-PM) into poly-cc, p-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA) and poly-α, β-[N-(2-aminoethyl)-L-aspartamide] (PAEA). The macromolecular ligands thus obtained were further complexed with gadolinium chloride to give macromolecular MRI contrast agents with different Gd(Ⅲ) contents. These macromolecular ligands and their gadolinium complexes were characterized by 1H NMR, 1R, UV and elementary analysis. Relaxivity studies showed that these polyaspartamide gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of the liver in rats and experimental data of biodistribution in mice indicate that these macromolecular MRI contrast agents containing pyridoxamine exhibit liver-targeting property. 相似文献
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