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J Cereb Blood Flow Metab. 2010 Mar;30(3):510-5. doi: 10.1038/jcbfm.2009.265. Epub 2009 Dec 16.

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

Author information

1
Department of Clinical Pharmacology, Medical University of Vienna, Vienna 1090, Austria.

Abstract

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.

PMID:
20010957
PMCID:
PMC2949150
DOI:
10.1038/jcbfm.2009.265
[Indexed for MEDLINE]
Free PMC Article

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