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

…, M Cdebaca, S Robinson, D Casebier

Index: Radeke, Heike S.; Purohit, Ajay; Harris, Thomas D.; Hanson, Kelley; Jones, Reinaldo; Hu, Carol; Yalamanchili, Padmaja; Hayes, Megan; Yu, Ming; Guaraldi, Mary; Kagan, Mikhail; Azure, Michael; Cdebaca, Michael; Robinson, Simon; Casebier, David ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 9 p. 650 - 655

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Citation Number: 5

Abstract

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 ...