| 研究実績の概要 |
An important clinical PET application is in myocardial perfusion imaging (MPI) for heart disease. The aim of this research was to synthesize and evaluate new 67/68Ga-complexes for PET myocardial-perfusion imaging.
We studied two separate classes of new hexadentate chelates (N4S2 and N4O2) that can easily be modified with substituents, provide stable complexation of Ga(III), and result in lipophilic, monocationic [Ga-complexes]+, properties necessary for myocardial uptake. Ligands for both chelate classes were synthesized and their Ga-complexes provided mono-cationic Ga-complexes. Radiolabeling with 67Ga(III) achieved high radiochemical yield in 30 min. In-vivo studies in normal mice display in-vivo stability, rapid distribution and clearance with low myocardial uptake due to lower lipophilicity compared to other known MPI agents (MIBI). While these chelates provided the desired stable Ga-complexes, further modifications for increased lipophilicity and improved myocardial retention are required to attain a effective PET myocardial perfusion agent with high myocardial uptake.
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