Warning: Undefined array key "mm" in /www/wwwroot/www.ai-bt.com/si.php on line 10 Deprecated: trim(): Passing null to parameter #1 ($string) of type string is deprecated in /www/wwwroot/www.ai-bt.com/si.php on line 10 Synthesis and Cardiac Imaging of (18)F-Ligands Selective for β1-Adrenoreceptors.

Literature DB >> 24900360

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

Heike S Radeke¹, Ajay Purohit¹, Thomas D Harris¹, Kelley Hanson¹, Reinaldo Jones¹, Carol Hu¹, Padmaja Yalamanchili¹, Megan Hayes¹, Ming Yu¹, Mary Guaraldi¹, Mikhail Kagan¹, Michael Azure¹, Michael Cdebaca¹, Simon Robinson¹, David Casebier¹.

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.

Entities: Chemical Gene Species

Keywords: 18F-labeling; PET; cardiac imaging; heart failure; β1-selective ligand

Year: 2011 PMID： 24900360 PMCID： PMC4018132 DOI： 10.1021/ml1002458

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

Keyword Cloud
References

22 in total

Review 1. PET and SPET tracers for mapping the cardiac nervous system.

Authors: Oliver Langer; Christer Halldin
Journal: Eur J Nucl Med Mol Imaging Date: 2002-03 Impact factor: 9.236

2. Preclinical evaluation of an 18F-labelled beta1-adrenoceptor selective radioligand based on ICI 89,406.

Authors: Marilyn P Law; Stefan Wagner; Klaus Kopka; Christiane Renner; Victor W Pike; Otmar Schober; Michael Schäfers
Journal: Nucl Med Biol Date: 2010-05 Impact factor: 2.408

3. Myocardial beta-adrenoceptor downregulation in idiopathic dilated cardiomyopathy measured in vivo with PET using the new radioligand (S)-[11C]CGP12388.

Authors: Richard M de Jong; Antoon T M Willemsen; Riemer H J A Slart; Paul K Blanksma; Aren van Waarde; Jan Hein Cornel; Willem Vaalburg; Dirk J van Veldhuisen; Philip H Elsinga
Journal: Eur J Nucl Med Mol Imaging Date: 2004-12-11 Impact factor: 9.236

4. Clinical, electrocardiographic, and hemodynamic effects of ICI 89,406, a new cardioselective beta-adrenoceptor antagonist with intrinsic sympathomimetic activity, in patients with angina pectoris.

Authors: P A Majid; J E Schreuder; P J de Feyter; J P Roos
Journal: J Cardiovasc Pharmacol Date: 1980 Jul-Aug Impact factor: 3.105

10. New approach for the synthesis of [18F]fluoroethyltyrosine for cancer imaging: simple, fast, and high yielding automated synthesis.

Authors: M Zuhayra; A Alfteimi; C Von Forstner; U Lützen; B Meller; E Henze
Journal: Bioorg Med Chem Date: 2009-09-20 Impact factor: 3.641

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

Review 1. PET and SPET tracers for mapping the cardiac nervous system.

2. Preclinical evaluation of an 18F-labelled beta1-adrenoceptor selective radioligand based on ICI 89,406.

3. Myocardial beta-adrenoceptor downregulation in idiopathic dilated cardiomyopathy measured in vivo with PET using the new radioligand (S)-[11C]CGP12388.

4. Clinical, electrocardiographic, and hemodynamic effects of ICI 89,406, a new cardioselective beta-adrenoceptor antagonist with intrinsic sympathomimetic activity, in patients with angina pectoris.

Review 5. Fundamental considerations of beta-adrenoceptor subtypes in human heart failure.

Review 6. Cardiac adrenoceptors: physiological and pathophysiological relevance.

7. Alterations in cardiac alpha and beta adrenoceptors during the development of spontaneous hypertension.

8. Design of new beta1-selective adrenoceptor ligands as potential radioligands for in vivo imaging.

9. Are [O-methyl-11C]derivatives of ICI 89,406 beta1-adrenoceptor selective radioligands suitable for PET?

10. New approach for the synthesis of [18F]fluoroethyltyrosine for cancer imaging: simple, fast, and high yielding automated synthesis.