Synthesis and Cardiac Imaging of (18)F-Ligands Selective for β1-Adrenoreceptors.
Radeke HS, Purohit A, Harris TD, Hanson K, Jones R, Hu C, Yalamanchili P, Hayes M, Yu M, Guaraldi M, Kagan M, Azure M, Cdebaca M, Robinson S, Casebier D.
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.