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- W2009169076 abstract "Using positron emission tomography (PET) imaging we assessed, in vivo, the interaction between a microdose of (R)-[11C]verapamil (a P-glycoprotein (Pgp) substrate) and escalating doses of the Pgp inhibitor tariquidar (3, 4, 6, and 8 mg/kg) at the blood–brain barrier (BBB) in healthy human subjects. We compared the dose–response relationship of tariquidar in humans with data obtained in rats using a similar methodology. Tariquidar was equipotent in humans and rats in its effect of increasing (R)-[11C]verapamil brain uptake (expressed as whole-brain volume of distribution (VT)), with very similar half-maximum-effect concentrations. Both in humans and in rats, brain VT approached plateau levels at plasma tariquidar concentrations >1,000 ng/ml. However, Pgp inhibition in humans led to only a 2.7-fold increase in brain VT relative to baseline scans (before administration of tariquidar) as compared with 11.0-fold in rats. The results of this translational study add to the accumulating evidence that there are marked species-dependent differences in Pgp expression and functionality at the BBB. Clinical Pharmacology & Therapeutics (2012); 91 2, 227–233. doi:10.1038/clpt.2011.217" @default.
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- W2009169076 date "2011-12-14" @default.
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- W2009169076 title "Pgp-Mediated Interaction Between (R)-[11C]Verapamil and Tariquidar at the Human Blood–Brain Barrier: A Comparison With Rat Data" @default.
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- W2009169076 doi "https://doi.org/10.1038/clpt.2011.217" @default.
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