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@ARTICLE{Hoffmann:1037540,
      author       = {Hoffmann, Chris and Endepols, Heike and Urusova, Elizaveta
                      and Elchine, Dominik and Neumaier, Felix and Neumaier, Bernd
                      and Zlatopolskiy, Boris},
      title        = {[18{F}]{R}91150: {I}mproved radiosynthesis and in vivo
                      evaluation as imaging probe for 5-{HT}2{A} receptors},
      journal      = {European journal of medicinal chemistry},
      volume       = {286},
      issn         = {0009-4374},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier Science},
      reportid     = {FZJ-2025-00729},
      pages        = {117265},
      year         = {2025},
      note         = {This work was supported by Deutsche Forschungsgemeinschaft
                      (DFG) grants ZL 65/1-1, ZL 65/3-1 and ZL 65/4-1.},
      abstract     = {Serotonergic 5-HT2A receptors in the cortex and other
                      forebrain structures have been linked to cognitive,emotional
                      and memory processes. In addition, dysfunction or altered
                      expression of these receptors is associatedwith
                      neuropsychiatric and neurodegenerative disorders.
                      [18F]R91150 is a candidate radiotracer for positronemission
                      tomography (PET) imaging of 5-HT2A receptors, which showed
                      promising properties in in vitro studies.However, existing
                      methods for the production of [18F]R91150 are rather
                      inefficient and its imaging propertieshave not been studied
                      in vivo. In the present work, we describe improved protocols
                      for preparation of[18F]R91150, the corresponding reference
                      compound and two alternative boronate radiolabeling
                      precursors.Furthermore, we present the results of an in vivo
                      evaluation of the radioligand in rodents. [18F]R91150
                      wasprepared in activity yields of 20 ± $5\%$ (two-step
                      radiosynthesis) or 12 ± $2\%$ (one-step radiosynthesis) and
                      withmolar activities of >200 GBq/μmol. μPET measurements
                      in mice revealed sufficient stability against in
                      vivodefluorination and predominantly hepatobiliary excretion
                      of the tracer, with high radioactivity uptake in gallbladder
                      and intestines. μPET imaging in rats demonstrated specific
                      tracer accumulation in the cortex andsubcortical forebrain
                      structures, which could be reduced by pretreatment or
                      displacement with the 5-HT2A receptorligands altanserin or
                      ketanserin but was insensitive to pretreatment with the
                      5-HT2C receptor ligandSB242084. In addition, [18F]R91150
                      showed specific accumulation in the choroid plexus that was
                      much lesssensitive to displacement with ketanserin and
                      unaffected by pretreatment with altanserin or SB242084.
                      Takentogether, our results indicate that [18F]R91150 may be
                      a promising candidate for in vivo PET imaging of
                      cortical5-HT2A receptors, although further studies will be
                      required to elucidate the mechanisms underlying
                      traceraccumulation in the choroid plexus.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {39826488},
      UT           = {WOS:001404938800001},
      doi          = {10.1016/j.ejmech.2025.117265},
      url          = {https://juser.fz-juelich.de/record/1037540},
}