Radioligands targeting P-glycoprotein and other drug efflux proteins at the blood-brain barrier. (Q38166961)

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1 March 2020

title

Radioligands targeting P-glycoprotein and other drug efflux proteins at the blood-brain barrier (English)

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1 March 2020

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1 March 2020

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1 March 2020

Thomas Wanek

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1 March 2020

language of work or name

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1 March 2013

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Journal of Labelled Compounds and Radiopharmaceuticals

1 March 2020

published in

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1 March 2020

volume

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issue

3-4

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1 March 2020

page(s)

68-77

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PET radiotracers: crossing the blood-brain barrier and surviving metabolism

1 March 2020

cites work

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Role of drug efflux transporters in the brain for drug disposition and treatment of brain diseases

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P-glycoprotein deficiency at the blood-brain barrier increases amyloid-beta deposition in an Alzheimer disease mouse model

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Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor

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Evaluation of tracer kinetic models for quantification of P-glycoprotein function using (R)-[11C]verapamil and PET.

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Pgp-mediated interaction between (R)-[11C]verapamil and tariquidar at the human blood-brain barrier: a comparison with rat data

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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

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P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide

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The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).

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Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs.

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Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomography

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Quantitative assessment of P-glycoprotein function in the rat blood-brain barrier by distribution volume of [11C]verapamil measured with PET.

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Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography

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Fully automated high yield synthesis of (R)- and (S)-[11C]verapamil for measuring P-glycoprotein function with positron emission tomography

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21 January 2018

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Synthesis and preclinical evaluation of [11C]D617, a metabolite of (R)-[11C]verapamil

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Evaluation of (R)-[11C]verapamil as PET tracer of P-glycoprotein function in the blood-brain barrier: kinetics and metabolism in the rat.

21 January 2018

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A novel positron emission tomography imaging protocol identifies seizure-induced regional overactivity of P-glycoprotein at the blood-brain barrier

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Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET.

21 January 2018

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Blood-brain barrier P-glycoprotein function in Alzheimer's disease

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Pharmacoresistance in epilepsy: a pilot PET study with the P-glycoprotein substrate R-[(11)C]verapamil

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Effect of age on functional P-glycoprotein in the blood-brain barrier measured by use of (R)-[(11)C]verapamil and positron emission tomography

21 January 2018

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11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux

21 January 2018

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Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function

21 January 2018

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P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeys

21 January 2018

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Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET

21 January 2018

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Effects of ketoconazole on the biodistribution and metabolism of [11C]loperamide and [11C]N-desmethyl-loperamide in wild-type and P-gp knockout mice

21 January 2018

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High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635.

21 January 2018

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Highlighting the Versatility of the Tracerlab Synthesis Modules. Part 1: Fully Automated Production of [F]Labelled Radiopharmaceuticals using a Tracerlab FX(FN).

21 January 2018

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Uptake and binding of the serotonin 5-HT1A antagonist [18F]-MPPF in brain of rats: effects of the novel P-glycoprotein inhibitor tariquidar

21 January 2018

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

21 January 2018

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Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives

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Synthesis and preclinical evaluation of novel PET probes for P-glycoprotein function and expression.

21 January 2018

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The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein

21 January 2018

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Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET.

21 January 2018

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Breast cancer resistance protein and P-glycoprotein in brain cancer: two gatekeepers team up

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

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A comparative small-animal PET evaluation of [11C]tariquidar, [11C]elacridar and (R)-[11C]verapamil for detection of P-glycoprotein-expressing murine breast cancer

21 January 2018

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21 January 2018

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Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier

21 January 2018

1 reference

Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [(11)C]GF120918 by PET in mice

21 January 2018

1 reference

Radiosynthesis and in vivo evaluation of 1-[18F]fluoroelacridar as a positron emission tomography tracer for P-glycoprotein and breast cancer resistance protein

21 January 2018

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Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats

21 January 2018

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The influence of mass of [11C]-laniquidar and [11C]-N-desmethyl-loperamide on P-glycoprotein blockage at the blood-brain barrier

21 January 2018

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Kinetic analysis of the cooperation of P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp/Abcg2) in limiting the brain and testis penetration of erlotinib, flavopiridol, and mitoxantrone

21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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Identifiers

DOI

10.1002/JLCR.2993

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24285312%20AND%20SRC:MED&resulttype=core&format=json

1 March 2020

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