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Synthesis of 2‐[18F]Fluoro‐2‐deoxyisosorbide 5‐mononitrate and Assessment of Its in vivo Biodistribution as Determined by Dynamic Positron Emission Tomography (PET)
Authors:Dr. Nico Santschi  Dr. Stefan Wagner  Dr. Constantin Daniliuc  Dr. Sven Hermann  Prof. Dr. Michael Schäfers  Prof. Dr. Ryan Gilmour
Affiliation:1. Institut für Organische Chemie, Westf?lische Wilhelms‐Universit?t Münster, Corrensstra?e?40, 48149 Münster (Germany) www.uni‐muenster.de/Chemie.oc/gilmour/en/index.html;2. Excellence Cluster EXC 1003 “Cells in Motion”, Westf?lische Wilhelms‐Universit?t Münster, 48149 Münster (Germany);3. Klinik für Nuklearmedizin, Westf?lische Wilhelms‐Universit?t Münster, Albert‐Schweitzer‐Campus?1, 48149 Münster (Germany);4. European Institute of Molecular Imaging, Westf?lische Wilhelms‐Universit?t Münster, Waldeyerstra?e?15, 48149 Münster (Germany)
Abstract:Herein we disclose the synthesis of 2‐fluoro‐2‐deoxyisosorbide 5‐mononitrate (2F‐IS‐5MN), a fluorinated analogue of the commonly prescribed vasodilator isosorbide 5‐mononitrate (IS‐5MN). X‐ray structural data for IS‐5MN and its C2‐epimeric congener IM‐5MN are presented together with structural data for 2F‐IS‐5MN. Radioisotope labeling of 2F‐IS‐5MN has, for the first time, allowed observation of the in vivo biodistribution of this organic nitrate by means of dynamic positron emission tomography (PET) in wild‐type mice.
Keywords:biodistribution  dynamic PET  fluorine  organic nitrates  radiosynthesis
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