| Structure-Activity Relationship and Preclinical Evaluation of Carbon-11-Labeled Ammonium Salts as PET-Myocardial Perfusion Imaging Agents. | |
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MedLine Citation:
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PMID: 22290562 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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BACKGROUND: Due to the limited availability of suitable positron emission tomography (PET) tracers, the majority of myocardial perfusion imaging (MPI) scans is performed using SPECT rather than PET. AIM: The aim of this study is to design and synthesize carbon-11-labeled ammonium salt derivatives and explore their structure-activity relationship (SAR) and their potential as PET-MPI agents. METHODS AND RESULTS: Three carbon-11-labeled ammonium salts were developed. SAR of the labeled compounds were explored vis-à-vis the effects of charge density and lipophilicity on the distribution kinetics in mice. These studies pointed at [(11)C]4 as the lead compound. Comparative microPET/CT scans in healthy rats, using both [(11)C]4 and [(13) N]-NH(3), substantiated the potential of [(11)C]4 ([(11)C]-DMDPA). A proof of concept for the potential of radiolabeled ammonium salts as MPI agents has been demonstrated in a newly developed swine model of permanent partial coronary artery occlusion. CONCLUSIONS: SAR studies of (11)C-labeled ammonium salts suggest that both lipophilicity and charge density affect the performance of these compounds as MPI probes. In a swine model, the labeled lead successfully visualized the defect regions in the myocardium. The data presented call for the development of fluorine-18 analogues, to increase clinical impact. |
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Authors:
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Ohad Ilovich; Galith Abourbeh; Moshe Bocher; Nanette Freedman; Hana Billauer; Sharon Dotan; Haim D Danenberg; Eyal Mishani |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-1-31 |
Journal Detail:
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Title: Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging Volume: - ISSN: 1860-2002 ISO Abbreviation: - Publication Date: 2012 Jan |
Date Detail:
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Created Date: 2012-1-31 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101125610 Medline TA: Mol Imaging Biol Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Cyclotron/Radiochemistry Unit/Nuclear Medicine Department, Hadassah Hebrew University Hospital, Jerusalem, 91120, Israel. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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