Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier

作者:Bauer Martin; Karch Rudolf; Neumann Friederike; Wagner Claudia C; Kletter Kurt; Mueller Markus; Loescher Wolfgang; Zeitlinger Markus; Langer Oliver*
来源:Journal of Cerebral Blood Flow and Metabolism, 2010, 30(3): 510-515.
DOI:10.1038/jcbfm.2009.265

摘要

` 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)[(11)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. Journal of Cerebral Blood Flow & Metabolism (2010) 30, 510-515; doi: 10.1038/jcbfm.2009.265; published online 16 December 2009

  • 出版日期2010-3