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- Title
Structure--activity relationship and preclinical evaluation of carbon-11-labeled ammonium salts as PET--myocardial perfusion imaging agents.
- Authors
Ilovich O; Abourbeh G; Bocher M; Freedman N; Billauer H; Dotan S; Danenberg HD; Mishani E; Ilovich, Ohad; Abourbeh, Galith; Bocher, Moshe; Freedman, Nanette; Billauer, Hana; Dotan, Sharon; Danenberg, Haim D; Mishani, Eyal
- Abstract
<bold>Background: </bold>Due to the limited availability of suitable positron emission tomography (PET) tracers, the majority of myocardial perfusion imaging (MPI) scans is performed using SPECT rather than PET.<bold>Aim: </bold>The aim of this study is to design and synthesize carbon-11-labeled ammonium salt derivatives and explore their structure–activity relationship (SAR) and their potential as PET–MPI agents.<bold>Methods and Results: </bold>Three carbon-11-labeled ammonium salts were developed. SAR of the labeled compounds were explored vis-à-vis the effects of charge density and lipophilicity on the distribution kinetics in mice. These studies pointed at [11C]4 as the lead compound. Comparative microPET/CT scans in healthy rats, using both [11C]4 and [13 N]–NH3, substantiated the potential of [11C]4 ([11C]-DMDPA). A proof of concept for the potential of radiolabeled ammonium salts as MPI agents has been demonstrated in a newly developed swine model of permanent partial coronary artery occlusion.<bold>Conclusions: </bold>SAR studies of 11C-labeled ammonium salts suggest that both lipophilicity and charge density affect the performance of these compounds as MPI probes. In a swine model, the labeled lead successfully visualized the defect regions in the myocardium. The data presented call for the development of fluorine-18 analogues, to increase clinical impact.
- Publication
Molecular Imaging & Biology, 2012, Vol 14, Issue 5, p625
- ISSN
1536-1632
- Publication type
journal article