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 …

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 …

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 …

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) …

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) …

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 …

Imaging of cyclosporine inhibition of P-glycoprotein activity using 11C-verapamil in the brain: studies of healthy humans

M Muzi, DA Mankoff, JM Link, S Shoner… - Journal of Nuclear …, 2009 - Soc Nuclear Med
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 …

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 …

Species differences in blood-brain barrier transport of three positron emission tomography radioligands with emphasis on P-glycoprotein transport

S Syvänen, Ö Lindhe, M Palner, BR Kornum… - Drug metabolism and …, 2009 - ASPET
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 …

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 …