Abstract
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)-[11 C]verapamil in five healthy volunteers during continuous intravenous tariquidar infusion. Total distribution volume (V T) of (R)-[11 C]verapamil in whole-brain gray matter increased by 273±78% relative to baseline scans without tariquidar, which was higher than previously reported V T increases. During tariquidar infusion whole-brain V T was comparable to V T in the pituitary gland, a region not protected by the BBB, which suggested that we were approaching complete Pgp inhibition at the human BBB.
Original language | English |
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Pages (from-to) | 743-746 |
Number of pages | 4 |
Journal | Journal of Cerebral Blood Flow and Metabolism |
Volume | 35 |
Issue number | 5 |
DOIs | |
Publication status | Published - 5 May 2015 |
Austrian Fields of Science 2012
- 301207 Pharmaceutical chemistry
Keywords
- (R)-[11C]verapamil
- blood-brain barrier
- P-glycoprotein
- pituitary gland
- positron emission tomography
- tariquidar