% IMPORTANT: The following is UTF-8 encoded.  This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.

@ARTICLE{Willmann:889311,
      author       = {Willmann, Michael and Ermert, Johannes and Prante, Olaf and
                      Hübner, Harald and Gmeiner, Peter and Neumaier, Bernd},
      title        = {{R}adiosynthesis and evaluation of 18{F}-labeled dopamine
                      {D}4-receptor ligands},
      journal      = {Nuclear medicine and biology},
      volume       = {92},
      issn         = {0969-8051},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier Science},
      reportid     = {FZJ-2021-00203},
      pages        = {43-52},
      year         = {2021},
      abstract     = {IntroductionThe dopamine D4 receptor (D4R) has attracted
                      considerable attention as potential target for the treatment
                      of a broad range of central nervous system disorders.
                      Although many efforts have been made to improve the
                      performance of putative radioligand candidates, there is
                      still a lack of D4R selective tracers suitable for in vivo
                      PET imaging. Thus, the objective of this work was to develop
                      a D4-selective PET ligand for clinical
                      applications.MethodsFour compounds based on previous and new
                      lead structures were prepared and characterized with regard
                      to their D4R subtype selectivity and predicted
                      lipophilicity. From these,
                      3-((4-(2-fluorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine
                      I and
                      (S)-4-(3-fluoro-4-methoxybenzyl)-2-(phenoxymethyl)morpholine
                      II were selected for labeling with fluorine-18 and
                      subsequent evaluation by in vitro autoradiography to assess
                      their suitability as D4 radioligand candidates for in vivo
                      imaging.ResultsThe radiosynthesis of [18F]I and [18F]II was
                      successfully achieved by copper-mediated radiofluorination
                      with radiochemical yields of $7\%$ and $66\%,$ respectively.
                      The radioligand [18F]II showed specific binding in areas
                      where D4 expression is expected, whereas [18F]I did not show
                      any uptake in distinct brain regions and exhibited an
                      unacceptable degree of non-specific binding.},
      cin          = {INM-5},
      ddc          = {570},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {525 - Decoding Brain Organization and Dysfunction
                      (POF4-525)},
      pid          = {G:(DE-HGF)POF4-525},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {32718750},
      UT           = {WOS:000616652500006},
      doi          = {10.1016/j.nucmedbio.2020.07.004},
      url          = {https://juser.fz-juelich.de/record/889311},
}