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@INPROCEEDINGS{Becker:150385,
      author       = {Becker, GA (Corresponding author) and Wilke, S and
                      Schönknecht, P and Patt, M and Luthardt, J and Hesse, S and
                      Meyer, PM and Barthel, H and Sorger, D and Seese, A and
                      Wagenknecht, Gudrun and Höpping, A and Fischer, S and
                      Brust, P and Sabri, O},
      title        = {{C}omparison of (-)-[18{F}]-{F}lubatine and
                      2-[18{F}]{FA}-85380 {B}inding to {N}icotinic alpha4beta2
                      {A}cetylcholine {R}eceptors in {H}uman {B}rains.},
      reportid     = {FZJ-2014-00446},
      year         = {2013},
      abstract     = {Aim: Nicotinic α4β2* acetylcholine receptors (nAChR) are
                      an important target for diagnostic neuroimaging because of
                      their involvement in Alzheimer's disease, Parkinson's
                      disease, tobacco and alcohol addiction. 2-[18F]FA-85380
                      (2-FA) has been used extensively for PET imaging of α4β2*
                      receptors but is limited as biomarker by its unfavourable
                      slow kinetic. The newly developed radiotracer
                      (-)-[18F]-Flubatine (Flubatine) shows a significantly
                      improved brain uptake, receptor affinity and selectivity
                      (1). Here we estimated the compartmental parameters of both
                      tracers by full kinetic modeling and compared them.
                      Materials and Methods: After intravenous administration of
                      ~370 MBq radiotracer PET brain imaging was performed in 20
                      healthy controls with Flubatine (age 70.6±4.6, scan
                      duration 90 min) and in 7 healthy controls with 2-FA (age
                      60.7±9.0, scan duration 420 min) using an ECAT EXACT HR+
                      system. PET frames were motion corrected with SPM2 and
                      kinetic modeling using a 1-tissue compartment model (1TCM)
                      with arterial input-function was applied to the volume of
                      interest (VOI) based tissue time-activity curves (TACs)
                      generated for 29 brain regions (anatomically defined via MRI
                      co-registration). The model-based receptor parameter used
                      was the total distribution volume VT (ml/cm3), tracer uptake
                      was measured by K1 (ml/cm3/min) and tracer tissue clearance
                      by k2 (1/min). Results: For both tracers TACs of all 29
                      brain regions could be described appropriately with the 1TCM
                      and all kinetic parameters could be reliably estimated from
                      the PET data. Regional VT increased as expected with
                      regional nAChR density. Parameters of Flubatine in
                      characteristic regions with very low, medium and high
                      receptor density were: Corpus callosum (K1= 0.18±0.04, k2=
                      0.032±0.004, VT= 5.68±1.01), Frontal cortex (K1=
                      0.37±0.04, k2= 0.040±0.003, VT= 9.18±0.59), Thalamus (K1=
                      0.48±0.06, k2= 0.020±0.003, VT= 25.03±3.33). The
                      respective parameters of 2-FA were: Corpus callosum (K1=
                      0.063±0.009, k2= 0.014±0.003, VT= 4.45±0.65), Frontal
                      cortex (K1= 0.099±0.013, k2= 0.018±0.001, VT= 5.42±0.56),
                      Thalamus (K1= 0.13±0.019, k2= 0.010±0.001, VT=
                      13.06±2.62). Conclusions: Flubatine is superior to 2-FA in
                      tracer uptake velocity (characterized by K1), velocity of
                      washout (characterized by k2) and in the amount of measured
                      specific binding (characterized by VT-target -
                      VT-reference). It shows a threefold higher uptake rate
                      constant K1 and a twofold higher washout rate constant k2,
                      providing the rational for much shorter scan durations in
                      case of Flubatine. These results are in good agreement with
                      our former findings in an animal (pig) model (1). Reference:
                      1. P. Brust, ..O. Sabri: In vivo measurement of nicotinic
                      acetylcholine receptors with
                      [18F]Norchloro-Fluoro-Homoepibatidine (Flubatine). Synapse
                      2008;62:205-218.},
      month         = {Oct},
      date          = {2013-10-19},
      organization  = {Annual Congress of the European
                       Association of Nuclear Medicine, Lyon
                       (France), 19 Oct 2013 - 23 Oct 2013},
      subtyp        = {Other},
      cin          = {ZEA-2},
      cid          = {I:(DE-Juel1)ZEA-2-20090406},
      pnm          = {332 - Imaging the Living Brain (POF2-332) / BMBF-01EZ0822 -
                      NorChloro-Fluoro HomoEpiBatidin (NCFHEB) ein potentieller
                      Positronen-Emission Tomographie-(PET) Marker der frühen
                      Alzheimer-Demenz (BMBF-01EZ0822) / NikotinPET - Validierung
                      von (+)-[18F]Flubatine als PET-Radiotracer zur Untersuchung
                      von Nikotinrezeptoren bei Demenz (HGF-HVF-0012)},
      pid          = {G:(DE-HGF)POF2-332 / G:(DE-Juel1)BMBF-01EZ0822 /
                      G:(DE-Juel1)HGF-HVF-0012},
      typ          = {PUB:(DE-HGF)24},
      url          = {https://juser.fz-juelich.de/record/150385},
}