| Literature DB >> 26796795 |
Barbara Wenzel1, Jan Mollitor2, Winnie Deuther-Conrad1, Sladjana Dukic-Stefanovic1, Mathias Kranz1, Chrysoula Vraka3, Rodrigo Teodoro1, Robert Günther1, Cornelius K Donat1, Friedrich-Alexander Ludwig1, Steffen Fischer1, Rene Smits2, Wolfgang Wadsak3, Markus Mitterhauser3, Jörg Steinbach1, Alexander Hoepping2, Peter Brust1.
Abstract
With the aim of imaging and quantification of oxytocin receptors (OTRs) in living brain using positron emission tomography (PET), we developed a (18)F-labeled small molecule radiotracer and investigated its in vivo pharmacokinetics in mice and pig. [(18)F]6b (KD = 12.3 nM) was radiolabeled by a two-step procedure using a microwave system with radiochemical yields of 26.9 ± 4.7%. Both organ distribution and small animal PET studies revealed limited brain uptake of [(18)F]6b in mouse (mean SUV of 0.04 at 30 min pi). Besides, significant radioactivity uptake in the pituitary gland was observed (SUV of 0.7 at 30 min pi). In a dynamic PET study in one piglet, we detected a higher uptake of [(18)F]6b in the olfactory bulb (SUV of 0.34 at 30 min pi) accompanied by a low uptake in the whole brain. In vitro autoradiographic studies on porcine brain sections indicated interaction of [(18)F]6b with several off-target receptors.Entities:
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Year: 2016 PMID： 26796795 DOI： 10.1021/acs.jmedchem.5b01080
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446