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@ARTICLE{Zlatopolskiy:842597,
      author       = {Zlatopolskiy, Boris D. and Zischler, Johannes and Schäfer,
                      Dominique and Urusova, Elizaveta and Guliyev, Mehrab and
                      Bannykh, Olesia and Endepols, Heike and Neumaier, Bernd},
      title        = {{D}iscovery of 7-[ 18 {F}]{F}luorotryptophan as a {N}ovel
                      {P}ositron {E}mission {T}omography ({PET}) {P}robe for the
                      {V}isualization of {T}ryptophan {M}etabolism in {V}ivo},
      journal      = {Journal of medicinal chemistry},
      volume       = {61},
      number       = {1},
      issn         = {1520-4804},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {FZJ-2018-00810},
      pages        = {189 - 206},
      year         = {2018},
      abstract     = {Tryptophan and its metabolites are involved in different
                      physiological and pathophysiological processes.
                      Consequently, positron emission tomography (PET) tracers
                      addressing tryptophan metabolic pathways should allow the
                      detection of different pathologies like neurological
                      disorders and cancer. Herein we report an efficient method
                      for the preparation of fluorotryptophans labeled in
                      different positions with 18F and their biological
                      evaluation. 4-7-[18F]Fluorotryptophans ([18F]FTrps) were
                      prepared according to a modified protocol of
                      alcohol-enhanced Cu-mediated radiofluorination in $30-53\%$
                      radiochemical yields. In vitro experiments demonstrated high
                      cellular uptake of 4-7-[18F]FTrps in different tumor cell
                      lines. 4, 5-, and 6-[18F]FTrps, although stable in vitro,
                      suffered from rapid in vivo defluorination. In contrast,
                      7-[18F]FTrp demonstrated a high in vivo stability and
                      enabled a clear delineation of serotonergic areas and
                      melatonin-producing pineal gland in rat brains. Moreover
                      7-[18F]FTrp accumulated in different tumor xenografts in a
                      chick embryo CAM model. Thus, 7-[18F]FTrp represents a
                      highly promising PET probe for imaging of Trp metabolism.},
      cin          = {INM-5},
      ddc          = {540},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {573 - Neuroimaging (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:29053271},
      UT           = {WOS:000422810800011},
      doi          = {10.1021/acs.jmedchem.7b01245},
      url          = {https://juser.fz-juelich.de/record/842597},
}