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@ARTICLE{Willmann:892695,
      author       = {Willmann, Michael and Hegger, Julian and Neumaier, Bernd
                      and Ermert, Johannes},
      title        = {{R}adiosynthesis and {B}iological {E}valuation of
                      [18{F}]{R}91150, a {S}elective 5-{HT}2{A} {R}eceptor
                      {A}ntagonist for {PET}-{I}maging},
      journal      = {ACS medicinal chemistry letters},
      volume       = {12},
      number       = {5},
      issn         = {1948-5875},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {FZJ-2021-02273},
      pages        = {738 - 744},
      year         = {2021},
      abstract     = {Serotonergic 5-HT2A receptors in cortical and forebrain
                      regions are an important substrate for the neuromodulatory
                      actions of serotonin in the brain. They have been implicated
                      in the etiology of many neuropsychiatric disorders and serve
                      as a target for antipsychotic, antidepressant, and
                      anxiolytic drugs. Positron emission tomography imaging using
                      suitable radioligands can be applied for in vivo
                      quantification of receptor densities and receptor occupancy
                      for therapy evaluation. Recently, the radiosynthesis of the
                      selective 5-HT2AR antagonist [18F]R91150 was reported.
                      However, the six-step radiosynthesis is cumbersome and
                      time-consuming with low radiochemical yields (RCYs) of
                      $<5\%.$ In this work, [18F]R91150 was prepared using
                      late-stage Cu-mediated radiofluorination to simplify its
                      synthesis. The detailed protocol enabled us to obtain RCYs
                      of 14 ± $1\%,$ and the total synthesis time was reduced to
                      60 min. In addition, autoradiographic studies with
                      [18F]R91150 in rat brain slices revealed the typical uptake
                      pattern of 5-HT2A receptor ligands.},
      cin          = {INM-5},
      ddc          = {610},
      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       = {34055220},
      UT           = {WOS:000651790900010},
      doi          = {10.1021/acsmedchemlett.0c00658},
      url          = {https://juser.fz-juelich.de/record/892695},
}