Interaction of 11C-tariquidar and 11C-elacridar with P-glycoprotein and breast cancer resistance protein at the human blood–brain barrier

M Bauer, R Karch, M Zeitlinger, J Stanek… - Journal of Nuclear …, 2013 - Soc Nuclear Med
The adenosine triphosphate-binding cassette transporters P-glycoprotein (Pgp) and breast
cancer resistance protein (BCRP) are 2 major gatekeepers at the blood–brain barrier (BBB) …

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 …

Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening

N Tournier, H Valette, MA Peyronneau… - Journal of Nuclear …, 2011 - Soc Nuclear Med
Radiolabeled compounds used for brain imaging with PET must readily cross the blood–
brain barrier (BBB) to reach their target. Efflux transporters at the BBB—P-glycoprotein (P …

Radioligands targeting P‐glycoprotein and other drug efflux proteins at the blood–brain barrier

T Wanek, S Mairinger, O Langer - Journal of Labelled …, 2013 - Wiley Online Library
Brain penetration of radiopharmaceuticals or therapeutic drugs may be restricted by
adenosine triphosphate‐binding cassette (ABC) transporters, such as P‐glycoprotein (Pgp) …

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 …

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 …

Synthesis and in vivo evaluation of the putative breast cancer resistance protein inhibitor [11C] methyl 4-((4-(2-(6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinolin-2-yl) …

S Mairinger, O Langer, C Kuntner, T Wanek… - Nuclear medicine and …, 2010 - Elsevier
INTRODUCTION: The multidrug efflux transporter breast cancer resistance protein (BCRP)
is highly expressed in the blood-brain barrier (BBB), where it limits brain entry of a broad …

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 …

A novel PET protocol for visualization of breast cancer resistance protein function at the blood–brain barrier

T Wanek, C Kuntner, JP Bankstahl… - Journal of cerebral …, 2012 - journals.sagepub.com
Breast cancer resistance protein (BCRP) is the most abundant multidrug efflux transporter at
the human blood–brain barrier (BBB), restricting brain distribution of various drugs. In this …

Imaging the impact of the P-glycoprotein (ABCB1) function on the brain kinetics of metoclopramide

G Pottier, S Marie, S Goutal, S Auvity… - Journal of Nuclear …, 2016 - Soc Nuclear Med
The effects of metoclopramide on the central nervous system (CNS) in patients suggest
substantial brain distribution. Previous data suggest that metoclopramide brain kinetics may …