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@ARTICLE{Humpert:1026004,
      author       = {Humpert, Swen and Schneider, Daniela and Lang, Markus and
                      Schulze, Annette and Neumaier, Felix and Holschbach, Marcus
                      and Bier, Dirk and Neumaier, Bernd},
      title        = {{R}adiosynthesis and {I}n {V}itro {E}valuation of
                      [11{C}]tozadenant as {A}denosine {A}2{A} {R}eceptor
                      {R}adioligand},
      journal      = {Molecules},
      volume       = {29},
      number       = {5},
      issn         = {1420-3049},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {FZJ-2024-03260},
      pages        = {1089},
      year         = {2024},
      abstract     = {Tozadenant
                      (4-hydroxy-N-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide)
                      is a highly selective adenosine A2A receptor (A2AR)
                      antagonist and a promisinglead structure for the development
                      of A2AR-selective positron emission tomography (PET)
                      probes.Although several 18F-labelled tozadenant derivatives
                      showed favorable in vitro properties, recentin vivo PET
                      studies observed poor brain penetration and lower specific
                      binding than anticipated fromthe in vitro data. While these
                      findings might be attributable to the structural
                      modification associatedwith 18F-labelling, they could also
                      reflect inherent properties of the parent compound.
                      However,PET studies with radioisotopologues of tozadenant to
                      evaluate its cerebral pharmacokinetics andbrain distribution
                      are still lacking. In the present work, we applied
                      N-Boc-O-desmethyltozadenantas a suitable precursor for the
                      preparation of [O-methyl-11C]tozadenant ([11C]tozadenant) by
                      Omethylationwith [11C]methyl iodide followed by acidic
                      deprotection. This approach afforded[11C]tozadenant in
                      radiochemical yields of 18 ± $2\%,$ with molar activities
                      of 50–60 GBq/μmol(1300–1600 mCi/μmol) and
                      radiochemical purities of 95 ± $3\%.$ In addition, in vitro
                      autoradiographyin pig and rat brain slices demonstrated the
                      expected striatal accumulation pattern and confirmedthe A2AR
                      specificity of the radioligand, making it a promising tool
                      for in vivo PET studies on thecerebral pharmacokinetics and
                      brain distribution of tozadenant.},
      cin          = {INM-5},
      ddc          = {540},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {38474602},
      UT           = {WOS:001183457000001},
      doi          = {10.3390/molecules29051089},
      url          = {https://juser.fz-juelich.de/record/1026004},
}