Assessment of Regional Differences in Tariquidar-Induced P-Glycoprotein Modulation at the Human Blood–Brain Barrier

  • Martin Bauer
    Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria
  • Rudolf Karch
    Department of Medical Statistics and Informatics, Medical University of Vienna, Vienna, Austria
  • Friederike Neumann
    Department of Medical Statistics and Informatics, Medical University of Vienna, Vienna, Austria
  • Claudia C Wagner
    Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria
  • Kurt Kletter
    Department of Nuclear Medicine, Medical University of Vienna, Vienna, Austria
  • Markus Müller
    Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria
  • Wolfgang Löscher
    Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine Hanover and Centre for Systems Neuroscience, Hanover, Germany
  • Markus Zeitlinger
    Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria
  • Oliver Langer
    Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria

抄録

<jats:p> We attempted to assess regional differences in cerebral P-glycoprotein (P-gp) function by performing paired positron emission tomography (PET) scans with the P-gp substrate ( R)-[<jats:sup>11</jats:sup>C]verapamil in five healthy subjects before and after i.v. infusion of tariquidar (2 mg/kg). Comparison of tariquidar-induced changes in distribution volumes ( DVs) in 42 brain regions of interest (ROIs) failed to detect significant differences among brain ROIs. Statistical parametric mapping analysis of parametric DV images visualized symmetrical bilateral clusters with moderately higher DV increases in response to tariquidar administration in cerebellum, parahippocampal gyrus, olfactory gyrus, and middle temporal lobe and cortex, which might reflect moderately decreased P-gp function and expression. </jats:p>

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