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

Autor:	Mikhail Kagan, Carol Hui Hu, Thomas D. Harris, Megan Hayes, Padmaja Yalamanchili, Kelley Hanson, Ming Yu, Michael Azure, Ajay Purohit, Simon P. Robinson, Reinaldo Jones, Michael Cdebaca, Mary Guaraldi, Radeke Heike S, David S. Casebier
Rok vydání:	2011
Předmět:	Pathology medicine.medical_specialty Lung Adrenergic receptor business.industry Blood pool Organic Chemistry Pharmacology medicine.disease Biochemistry medicine.anatomical_structure In vivo Heart failure Drug Discovery Medicine Tissue distribution business IC50 Cardiac imaging
Zdroj:	ACS Medicinal Chemistry Letters. 2:650-655
ISSN:	1948-5875
DOI:	10.1021/ml1002458
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::011363cd3addeb5ca8b13c5c85c2939e https://doi.org/10.1021/ml1002458 Zobrazit plný text záznamu