Preparation of new technetium-99m NNS/X complexes and selection for brain imaging agent

摘要

Based on excellent experiment results of 99mTcO-MPBDA-Cl, two new ligands MPTDA and MPDAA are synthesized. Then series of 99mTcO3+ complexes are prepared through adding different halide anions, followed by tests of physical chemistry qualities and biodistribution experiments. And results of these experiments show that complexes formed with MPTDA and MPDAA have better lipophilicity than those formed with MPBDA, still maintain the good brain retention ability of this type of compounds, but radioactivity uptake in blood is higher than that of 99m TcO-MPBDA and ratios of brain/blood are reduced. Obvious affections are fetched out on brain uptake and retention if fluoride, bromide or iodide anions are added. Results of experiments can be explained in reason with theoretic computation. It is confirmed that 99m TcO-MPBDA-Cl has potential to develop a new type of brain imaging agent considering integrated factors such as brain uptake, retention and toxicity.