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@ARTICLE{Sundheimer:300695,
      author       = {J. K. Sundheimer$^*$ and J. Benzel$^*$ and R.
                      Longuespée$^*$ and J. Burhenne and S. Pfister$^*$ and K.
                      Maass$^*$ and M. Sauter and K. Pajtler$^*$},
      title        = {{E}xperimental {I}nsights and {R}ecommendations for
                      {S}uccessfully {P}erforming {C}erebral {M}icrodialysis
                      {W}ith {H}ydrophobic {D}rug {C}andidates.},
      journal      = {Clinical and translational science},
      volume       = {18},
      number       = {5},
      issn         = {1752-8054},
      address      = {Oxford},
      publisher    = {Wiley-Blackwell},
      reportid     = {DKFZ-2025-00875},
      pages        = {e70226},
      year         = {2025},
      note         = {#EA:B062#LA:B062#},
      abstract     = {Cerebral microdialysis in rodents represents a robust and
                      versatile technique for quantifying the pharmacologically
                      relevant unbound fraction of drugs in the brain. When this
                      unbound fraction is simultaneously determined in plasma, it
                      facilitates the calculation of the corresponding unbound
                      plasma-to-brain partition coefficient (Kp,uu) for a given
                      compound in vivo. This coefficient is critical for
                      understanding the penetration and distribution of drugs
                      across the blood-brain barrier (BBB). However, obtaining
                      valid and accurate microdialysis data can be particularly
                      challenging for hydrophobic drugs due to their pronounced
                      non-specific interactions with the components of the
                      microdialysis system. The present study reports the outcomes
                      of comprehensive microdialysis investigations in rodents,
                      focusing on three hydrophobic compounds: actinomycin D,
                      selinexor, and ulixertinib. These compounds exhibited
                      varying degrees of non-specific binding to the surfaces of
                      the microdialysis apparatus, leading to low recovery rates
                      and substantial carry-over effects. To diminish these
                      limitations, strategies such as surface coating and the use
                      of optimized materials were employed to enhance the
                      reliability of the microdialysis system. To ensure the
                      robustness and reproducibility of microdialysis-related
                      research outcomes, our experimental findings were
                      supplemented with a narrative literature review. This review
                      encompassed keyword-driven PubMed-indexed publications on
                      microdialysis from 1970 to 2024, providing a broader context
                      for the challenges and solutions associated with the
                      technique. By integrating empirical results with practical
                      recommendations, this study offers a comprehensive resource
                      aimed at advancing the application of cerebral microdialysis
                      in preclinical drug development, particularly for compounds
                      with challenging physicochemical properties.},
      subtyp        = {Review Article},
      keywords     = {Microdialysis: methods / Microdialysis: instrumentation /
                      Animals / Blood-Brain Barrier: metabolism / Hydrophobic and
                      Hydrophilic Interactions / Brain: metabolism /
                      Reproducibility of Results / Rats / Humans / Mice / central
                      nervous system (Other) / cerebral microdialysis (Other) /
                      chemical drug properties (Other) / non‐specific binding
                      (Other) / probe implantation (Other)},
      cin          = {B062 / HD01 / B350},
      ddc          = {610},
      cid          = {I:(DE-He78)B062-20160331 / I:(DE-He78)HD01-20160331 /
                      I:(DE-He78)B350-20160331},
      pnm          = {312 - Funktionelle und strukturelle Genomforschung
                      (POF4-312)},
      pid          = {G:(DE-HGF)POF4-312},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:40286321},
      pmc          = {pmc:PMC12033007},
      doi          = {10.1111/cts.70226},
      url          = {https://inrepo02.dkfz.de/record/300695},
}