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SAGE Publications, Journal of Cerebral Blood Flow and Metabolism, 3(30), p. 510-515, 2009

DOI: 10.1038/jcbfm.2009.265

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

This paper is available in a repository.
This paper is available in a repository.

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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)-[11C]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.