scholarly journals P-Glycoprotein Function at the Blood–Brain Barrier: Effects of Age and Gender

2012 ◽  
Vol 14 (6) ◽  
pp. 771-776 ◽  
Author(s):  
Daniëlle M. E. van Assema ◽  
Mark Lubberink ◽  
Ronald Boellaard ◽  
Robert C. Schuit ◽  
Albert D. Windhorst ◽  
...  
2015 ◽  
Vol 35 (5) ◽  
pp. 743-746 ◽  
Author(s):  
Martin Bauer ◽  
Rudolf Karch ◽  
Markus Zeitlinger ◽  
Cécile Philippe ◽  
Kerstin Römermann ◽  
...  

As P-glycoprotein (Pgp) inhibition at the blood–brain barrier (BBB) after administration of a single dose of tariquidar is transient, we performed positron emission tomography (PET) scans with the Pgp substrate ( R)-[11C]verapamil in five healthy volunteers during continuous intravenous tariquidar infusion. Total distribution volume ( VT) of ( R)-[11C]verapamil in whole-brain gray matter increased by 273 ± 78% relative to baseline scans without tariquidar, which was higher than previously reported VT increases. During tariquidar infusion whole-brain VT was comparable to VT in the pituitary gland, a region not protected by the BBB, which suggested that we were approaching complete Pgp inhibition at the human BBB.


2007 ◽  
pp. 671-700
Author(s):  
Mahalia S. Desruisseaux ◽  
Louis M. Weiss ◽  
Herbert B. Tanowitz ◽  
Adam Mott ◽  
Danny A. Milner

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