Pillai M R, Kothari K, Mathew B, Pilkwal N K, Jurisson S
Radiopharmaceuticals Section, Bhabha Atomic Research Centre, Mumbai, India.
Nucl Med Biol. 1999 Feb;26(2):233-8. doi: 10.1016/s0969-8051(98)00102-4.
Heptadentate amine-phenol ligands with N4O3 donor atoms for coordination were synthesized by condensing tris(2-aminoethyl)amine with salicylaldehyde or acetophenone and reducing the Schiff bases formed with NaBH4. The ligands were characterized by 1H and 13C nuclear magnetic resonance spectroscopy. Radiochemical studies were carried out with no-carrier-added 99mTc and 99mTc spiked with 0.1-100 microM of 99Tc. Complexation yields were estimated from thin layer chromatography, paper electrophoresis, and solvent extraction studies. 99mTc complexes were formed in yields better than 90% with the amine-phenol ligands. The complexes were found to be neutral and lipophilic. Biodistribution studies of the 99mTc complexes showed that clearance was mainly through the hepatobiliary system.
通过将三（2-氨基乙基）胺与水杨醛或苯乙酮缩合并用硼氢化钠还原形成的席夫碱，合成了具有N4O3供体原子用于配位的七齿胺-酚配体。通过1H和13C核磁共振光谱对配体进行了表征。使用无载体添加的99mTc和添加了0.1-100微摩尔99Tc的99mTc进行了放射化学研究。通过薄层色谱、纸电泳和溶剂萃取研究估算了络合产率。99mTc与胺-酚配体形成的络合物产率优于90%。发现这些络合物呈中性且具有亲脂性。99mTc络合物的生物分布研究表明，清除主要通过肝胆系统进行。
