Synthesis of 2-[(18)F]Fluoro-2-deoxyisosorbide 5-mononitrate and Assessment of Its in vivo Biodistribution as Determined by Dynamic Positron Emission Tomography (PET).
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.
Institut für Organische Chemie, Westfälische Wilhelms-Universität Münster, Corrensstraße 40, 48149 Münster (Germany) www.uni-muenster.de/Chemie.oc/gilmour/en/index.html.|Excellence Cluster EXC 1003 "Cells in Motion", Westfälische Wilhelms-Universität Münster, 48149 Münster (Germany).
Nico
N
Santschi
Klinik für Nuklearmedizin, Westfälische Wilhelms-Universität Münster, Albert-Schweitzer-Campus 1, 48149 Münster (Germany).
Stefan
S
Wagner
Institut für Organische Chemie, Westfälische Wilhelms-Universität Münster, Corrensstraße 40, 48149 Münster (Germany) www.uni-muenster.de/Chemie.oc/gilmour/en/index.html.
Constantin
C
Daniliuc
Excellence Cluster EXC 1003 "Cells in Motion", Westfälische Wilhelms-Universität Münster, 48149 Münster (Germany).|European Institute of Molecular Imaging, Westfälische Wilhelms-Universität Münster, Waldeyerstraße 15, 48149 Münster (Germany).
Sven
S
Hermann
Excellence Cluster EXC 1003 "Cells in Motion", Westfälische Wilhelms-Universität Münster, 48149 Münster (Germany). schafmi@uni-muenster.de.|Klinik für Nuklearmedizin, Westfälische Wilhelms-Universität Münster, Albert-Schweitzer-Campus 1, 48149 Münster (Germany). schafmi@uni-muenster.de.|European Institute of Molecular Imaging, Westfälische Wilhelms-Universität Münster, Waldeyerstraße 15, 48149 Münster (Germany). schafmi@uni-muenster.de.
Michael
M
Schäfers
Institut für Organische Chemie, Westfälische Wilhelms-Universität Münster, Corrensstraße 40, 48149 Münster (Germany) www.uni-muenster.de/Chemie.oc/gilmour/en/index.html. ryan.gilmour@uni-muenster.de.|Excellence Cluster EXC 1003 "Cells in Motion", Westfälische Wilhelms-Universität Münster, 48149 Münster (Germany). ryan.gilmour@uni-muenster.de.
Ryan
R
Gilmour
D000818:Animals; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007547:Isosorbide / Q000031:analogs & derivatives* / Q000032:analysis / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008958:Models, Molecular; D015394:Molecular Structure; D009566:Nitrates / Q000032:analysis* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography; D014018:Tissue Distribution
C000608762:2-fluoro-2-deoxyisosorbide 5-mononitrate; D005462:Fluorine Radioisotopes; D009566:Nitrates; D007547:Isosorbide
biodistribution; dynamic PET; fluorine; organic nitrates; radiosynthesis