Tariquidar-induced P-glycoprotein inhibition at the rat blood–brain barrier studied with (R)-11C-verapamil and PET
JP Bankstahl, C Kuntner, A Abrahim… - Journal of Nuclear …, 2008 - Soc Nuclear Med
The multidrug efflux transporter P-glycoprotein (P-gp) is expressed in high concentrations at
the blood–brain barrier (BBB) and is believed to be implicated in resistance to central …
the blood–brain barrier (BBB) and is believed to be implicated in resistance to central …
A pilot study to assess the efficacy of tariquidar to inhibit P-glycoprotein at the human blood–brain barrier with (R)-11C-verapamil and PET
CC Wagner, M Bauer, R Karch… - Journal of nuclear …, 2009 - Soc Nuclear Med
Tariquidar, a potent, nontoxic, third-generation P-glycoprotein (P-gp) inhibitor, is a possible
reversal agent for central nervous system drug resistance. In animal studies, tariquidar has …
reversal agent for central nervous system drug resistance. In animal studies, tariquidar has …
Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[11C]verapamil …
C Kuntner, JP Bankstahl, M Bankstahl, J Stanek… - European journal of …, 2010 - Springer
Purpose Overactivity of the multidrug efflux transporter P-glycoprotein (P-gp) at the blood-
brain barrier (BBB) is believed to play an important role in resistance to central nervous …
brain barrier (BBB) is believed to play an important role in resistance to central nervous …
Approaching Complete Inhibition of P-Glycoprotein at the Human Blood–Brain Barrier: An (R)-[11C]Verapamil PET Study
M Bauer, R Karch, M Zeitlinger… - Journal of Cerebral …, 2015 - journals.sagepub.com
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) …
single dose of tariquidar is transient, we performed positron emission tomography (PET) …
Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood–brain barrier
M Bauer, R Karch, F Neumann… - Journal of Cerebral …, 2010 - journals.sagepub.com
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) …
performing paired positron emission tomography (PET) scans with the P-gp substrate (R) …
Pgp‐Mediated Interaction Between (R)‐[11C]Verapamil and Tariquidar at the Human Blood–Brain Barrier: A Comparison With Rat Data
M Bauer, M Zeitlinger, R Karch… - Clinical …, 2012 - Wiley Online Library
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 …
between a microdose of (R)‐[11C] verapamil (a P‐glycoprotein (Pgp) substrate) and …
Imaging of cyclosporine inhibition of P-glycoprotein activity using 11C-verapamil in the brain: studies of healthy humans
The multiple-drug resistance (MDR) transporter P-glycoprotein (P-gp) is highly expressed at
the human blood–brain barrier (BBB). P-gp actively effluxes a wide variety of drugs from the …
the human blood–brain barrier (BBB). P-gp actively effluxes a wide variety of drugs from the …
Increased permeability-glycoprotein inhibition at the human blood–brain barrier can be safely achieved by performing PET during peak plasma concentrations of …
WC Kreisl, R Bhatia, CL Morse, AE Woock… - Journal of Nuclear …, 2015 - Soc Nuclear Med
The permeability-glycoprotein (P-gp) efflux transporter is densely expressed at the blood–
brain barrier, and its resultant spare capacity requires substantial blockade to increase the …
brain barrier, and its resultant spare capacity requires substantial blockade to increase the …
Species differences in blood-brain barrier transport of three positron emission tomography radioligands with emphasis on P-glycoprotein transport
Species differences occur in the brain concentrations of drugs, but the reasons for these
differences are not yet apparent. This study was designed to compare brain uptake of three …
differences are not yet apparent. This study was designed to compare brain uptake of three …
P-glycoprotein function at the blood–brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide
WC Kreisl, JS Liow, N Kimura, N Seneca… - Journal of Nuclear …, 2010 - Soc Nuclear Med
Permeability-glycoprotein (P-gp), an efflux transporter in several organs, acts at the blood–
brain barrier to protect the brain from exogenous toxins. P-gp almost completely blocks brain …
brain barrier to protect the brain from exogenous toxins. P-gp almost completely blocks brain …
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