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@ARTICLE{Kroll:134641,
      author       = {Kroll, Tina and Elmenhorst, David and Matusch, Andreas and
                      Wedekind, Franziska and Weißhaupt, Angela and Beer, Simone
                      and Bauer, Andreas},
      title        = {{S}uitability of [18{F}]{A}ltanserin and {PET} to
                      {D}etermine 5-{HT}2{A} {R}eceptor {A}vailability in the
                      {R}at {B}rain: {I}n {V}ivo and {I}n {V}itro {V}alidation of
                      {I}nvasive and {N}on-{I}nvasive {K}inetic {M}odels},
      journal      = {Molecular imaging $\&$ biology},
      volume       = {15},
      number       = {4},
      issn         = {1860-2002},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier Science},
      reportid     = {FZJ-2013-02758},
      pages        = {456-467},
      year         = {2013},
      abstract     = {PURPOSE: While the selective 5-hydroxytryptamine type 2a
                      receptor (5-HT2AR) radiotracer [(18)F]altanserin is well
                      established in humans, the present study evaluated its
                      suitability for quantifying cerebral 5-HT2ARs with positron
                      emission tomography (PET) in albino rats. PROCEDURES: Ten
                      Sprague Dawley rats underwent 180 min PET scans with
                      arterial blood sampling. Reference tissue methods were
                      evaluated on the basis of invasive kinetic models with
                      metabolite-corrected arterial input functions. In vivo
                      5-HT2AR quantification with PET was validated by in vitro
                      autoradiographic saturation experiments in the same animals.
                      RESULT: Overall brain uptake of [(18)F]altanserin was
                      reliably quantified by invasive and non-invasive models with
                      the cerebellum as reference region shown by linear
                      correlation of outcome parameters. Unlike in humans, no
                      lipophilic metabolites occurred so that brain activity
                      derived solely from parent compound. PET data correlated
                      very well with in vitro autoradiographic data of the same
                      animals. CONCLUSION: [(18)F]Altanserin PET is a reliable
                      tool for in vivo quantification of 5-HT2AR availability in
                      albino rats. Models based on both blood input and reference
                      tissue describe radiotracer kinetics adequately. Low
                      cerebral tracer uptake might, however, cause restrictions in
                      experimental usage.},
      cin          = {INM-2 / ZEA-2},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-2-20090406 / I:(DE-Juel1)ZEA-2-20090406},
      pnm          = {333 - Pathophysiological Mechanisms of Neurological and
                      Psychiatric Diseases (POF2-333)},
      pid          = {G:(DE-HGF)POF2-333},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:23456885},
      UT           = {WOS:000321972500013},
      doi          = {10.1007/s11307-013-0621-3},
      url          = {https://juser.fz-juelich.de/record/134641},
}