Synthesis and Cardiac Imaging of 18F-Ligands Selective for β1-Adrenoreceptors

A series of potent and selective β1-adrenoreceptor ligands were identified (IC50 range, 0.04–0.25 nM; β1/β2 selectivity range, 65–450-fold), labeled with the PET radioisotope fluorine-18 and evaluated in normal Sprague–Dawley rats. Tissue distribution studies demonstrated uptake of each radiotracers from the blood pool into the myocardium (0.48–0.62% ID/g), lung (0.63–0.97% ID/g), and liver (1.03–1.14% ID/g). Dynamic μPET imaging confirmed the in vivo dissection studies.