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@ARTICLE{Leithold:279287,
      author       = {Leithold, Leonie H. E. and Jiang, Nan and Post, Julia and
                      Ziehm, Tamar and Schartmann, Elena and Kutzsche, Janine and
                      Shah, N. Jon and Breitkreutz, Jörg and Langen, Karl-Josef
                      and Willuweit, Antje and Willbold, Dieter},
      title        = {{P}harmacokinetic {P}roperties of a {N}ovel d-{P}eptide
                      {D}eveloped to be {T}herapeutically {A}ctive {A}gainst
                      {T}oxic β-{A}myloid {O}ligomers},
      journal      = {Pharmaceutical research},
      volume       = {33},
      number       = {2},
      issn         = {1573-904X},
      address      = {Dordrecht [u.a.]},
      publisher    = {Springer Science + Business Media B.V},
      reportid     = {FZJ-2015-07302},
      pages        = {328-36},
      year         = {2016},
      abstract     = {PURPOSE:It has been shown that amyloid β (Aβ) oligomers
                      play an important role in the pathology of Alzheimer's
                      disease (AD). D3, a peptide consisting solely of
                      D-enantiomeric amino acid residues, was developed to
                      specifically eliminate Aβ oligomers and is therapeutically
                      active in transgenic AD mice. D-peptides have several
                      advantages over L-peptides, but little is known about their
                      pharmacokinetic potential in vivo. Here, we analysed the
                      pharmacokinetic properties of RD2, a rationally designed and
                      potent D3 derivative.METHODS:The pharmacokinetic analysis
                      was performed using 3H-RD2 after administration via several
                      routes in mice. The time dependent amount of radiolabelled
                      RD2 was measured in plasma and several organ homogenates by
                      liquid scintillation counting. Furthermore, binding to
                      plasma proteins was estimated.RESULTS:RD2 penetrates into
                      the brain, where it is thought to implement its therapeutic
                      function. All administration routes result in a maximal
                      brain concentration per dose (Cmax/D) of 0.06
                      (μg/g)/(mg/kg) with brain/plasma ratios ranging between 0.7
                      and 1.0. RD2 shows a small elimination constant and a long
                      terminal half-life in plasma of more than 2 days. It also
                      exhibits high bioavailability after i.p., s.c. or p.o.
                      administration.CONCLUSIONS:These excellent pharmacokinetic
                      properties confirm that RD2 is a very promising drug
                      candidate for AD.KEYWORDS:Alzheimer’s disease;
                      D-enantiomer; peptide; pharmacokinetics; preclinical},
      cin          = {ICS-6 / INM-4},
      ddc          = {610},
      cid          = {I:(DE-Juel1)ICS-6-20110106 / I:(DE-Juel1)INM-4-20090406},
      pnm          = {553 - Physical Basis of Diseases (POF3-553)},
      pid          = {G:(DE-HGF)POF3-553},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000368073300007},
      pubmed       = {pmid:26381279},
      doi          = {10.1007/s11095-015-1791-2},
      url          = {https://juser.fz-juelich.de/record/279287},
}