title: Synthesis and Cardiac Imaging of (18)F-Ligands Selective for β1-Adrenoreceptors.
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 the in vivo dissection studies.
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Heike S
authors.initials: HS
authors.lastname: Radeke
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Ajay
authors.initials: A
authors.lastname: Purohit
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Harris
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Kelley
authors.initials: K
authors.lastname: Hanson
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Reinaldo
authors.initials: R
authors.lastname: Jones
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Carol
authors.initials: C
authors.lastname: Hu
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Padmaja
authors.initials: P
authors.lastname: Yalamanchili
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Megan
authors.initials: M
authors.lastname: Hayes
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Ming
authors.initials: M
authors.lastname: Yu
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Mary
authors.initials: M
authors.lastname: Guaraldi
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Mikhail
authors.initials: M
authors.lastname: Kagan
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Michael
authors.initials: M
authors.lastname: Azure
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Michael
authors.initials: M
authors.lastname: Cdebaca
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: Simon
authors.initials: S
authors.lastname: Robinson
authors.affiliation: Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
authors.forename: David
authors.initials: D
authors.lastname: Casebier
keywords: 18F-labeling; PET; cardiac imaging; heart failure; β1-selective ligand