Approaching Complete Inhibition of P-Glycoprotein at the Human Blood–Brain Barrier: An (R)-[11C]Verapamil PET Study
2015 ◽
Vol 35
(5)
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pp. 743-746
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Keyword(s):
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.
2001 ◽
Vol 41
(7)
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pp. 48-54
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2015 ◽
Vol 12
(9)
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pp. 3214-3225
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2001 ◽
Vol 41
(99)
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pp. 48-54
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2010 ◽
Vol 87
(5)
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pp. 579-585
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Keyword(s):
2016 ◽
Vol 37
(4)
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pp. 1286-1298
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2011 ◽
Vol 31
(24)
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pp. 8803-8811
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2005 ◽
Vol 77
(6)
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pp. 503-514
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2012 ◽
Vol 696
(1-3)
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pp. 18-27
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2008 ◽
Vol 37
(3)
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pp. 635-643
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