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


Bauer, M; Karch, R; Neumann, F; Wagner, C C; Kletter, K; Müller, M; Löscher, W; Zeitlinger, M; Langer, O (2010). Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier. Journal of Cerebral Blood Flow and Metabolism, 30(3):510-515.

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.

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.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:04 Faculty of Medicine > University Hospital Zurich > Clinic and Policlinic for Internal Medicine
Dewey Decimal Classification:610 Medicine & health
Language:English
Date:2010
Deposited On:15 Feb 2010 12:33
Last Modified:05 Apr 2016 13:54
Publisher:Nature Publishing Group
ISSN:0271-678X
Publisher DOI:10.1038/jcbfm.2009.265
PubMed ID:20010957

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