Evaluation of p-glycoprotein (abcb1a/b) modulation of [f-18]fallypride in micropet imaging studies

Publication type:
Journal article
Metadata:
Autoren
  • Markus Piel
  • Ulrich Schmitt
  • Nicole Bausbacher
  • Hans-Georg Buchholz
  • Gerhard Gruender
  • Christoph Hiemke
  • Frank Rösch
Sammlungen
  • metadata
ISSN
0028-3908
Zeitschrift
Neuropharmacology
Schlüsselwörter
  • 000 Allgemeines
  • 000 Generalities
Sprache
eng
Paginierung
Seiten: 152 - 158
Datum der Veröffentlichung
2014
Herausgeber
Elsevier
Herausgeber URL
http://dx.doi.org/10.1016/j.neuropharm.2013.04.062
Datum der Datenerfassung
2020
Datum, an dem der Datensatz öffentlich gemacht wurde
2020
Zugang
Public
Titel
Evaluation of p-glycoprotein (abcb1a/b) modulation of [f-18]fallypride in micropet imaging studies
Ausgabe der Zeitschrift
84

Data source: METADATA.UB

Other metadata sources:
Autoren
  • Markus Piel
  • Ulrich Schmitt
  • Nicole Bausbacher
  • Hans-Georg Buchholz
  • Gerhard Gruender
  • Christoph Hiemke
  • Frank Roesch
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000338616600016&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.1016/j.neuropharm.2013.04.062
eISSN
1873-7064
Externe Identifier
  • Clarivate Analytics Document Solution ID: AK7OC
  • PubMed Identifier: 23994301
ISSN
0028-3908
Zeitschrift
NEUROPHARMACOLOGY
Schlüsselwörter
  • [F-18]fallypride
  • Dopamine D-2/D-3 receptors
  • P-Glycoprotein
  • Cyclosporine A
  • Positron emission tomography
Paginierung
152 - 158
Datum der Veröffentlichung
2014
Status
Published
Titel
Evaluation of P-glycoprotein (abcb1a/b) modulation of [<SUP>18</SUP>F]fallypride in MicroPET imaging studies
Sub types
  • Article
Ausgabe der Zeitschrift
84

Data source: Web of Science (Lite)

Autoren
  • Markus Piel
  • Ulrich Schmitt
  • Nicole Bausbacher
  • Hans-Georg Buchholz
  • Gerhard Gründer
  • Christoph Hiemke
  • Frank Rösch
DOI
10.1016/j.neuropharm.2013.04.062
ISSN
0028-3908
Zeitschrift
Neuropharmacology
Sprache
en
Paginierung
152 - 158
Datum der Veröffentlichung
2014
Status
Published
Herausgeber
Elsevier BV
Herausgeber URL
http://dx.doi.org/10.1016/j.neuropharm.2013.04.062
Datum der Datenerfassung
2020
Titel
Evaluation of P-glycoprotein (abcb1a/b) modulation of [18F]fallypride in MicroPET imaging studies
Ausgabe der Zeitschrift
84

Data source: Crossref

Abstract
[(18)F]Fallypride ([(18)F]FP) is an important and routinely used D2/D3 antagonist for quantitative imaging of dopaminergic neurotransmission in vivo. Recently it was shown that the brain uptake of the structurally related [(11)C]raclopride is modulated by P-glycoprotein (P-gp), an important efflux transporter at the blood-brain barrier. The purpose of this study was to determine whether the brain uptake of [(18)F]FP is influenced by P-gp. For examination of this possible modulation microPET studies were performed in a rat and a mouse model. Hence, [(18)F]FP was applied to Sprague Dawley rats, half of them being treated with the P-gp inhibitor cyclosporine A (CsA). In a second experimental series the tracer was applied to three different groups of FVB/N mice: wild type, P-gp double knockout (abcb1a/1b (-/-)) and CsA-treated mice. In CsA-treated Sprague Dawley rats [(18)F]FP showed an elevated standard uptake value in the striatum compared to the control animals. In FVB/N mice a similar effect was observed, showing an increasing uptake from wild type to CsA-treated and double knockout mice. Since genetically or pharmacologically induced reduction of P-gp activity increased the uptake of [(18)F]FP markedly, we conclude that [(18)F]FP is indeed a substrate of P-gp and that the efflux pump modulates its brain uptake. This effect - if true for humans - may have particular impact on clinical studies using [(18)F]FP for assessment of D2/3 receptor occupancy by antipsychotic drugs. This article is part of the Special Issue Section entitled 'Neuroimaging in Neuropharmacology'.
Addresses
  • Institute of Nuclear Chemistry, Johannes Gutenberg-University, Fritz-Strassmann-Weg 2, D-55128 Mainz, Germany. Electronic address: piel@uni-mainz.de.
Autoren
  • Markus Piel
  • Ulrich Schmitt
  • Nicole Bausbacher
  • Hans-Georg Buchholz
  • Gerhard Gründer
  • Christoph Hiemke
  • Frank Rösch
DOI
10.1016/j.neuropharm.2013.04.062
eISSN
1873-7064
Externe Identifier
  • PubMed Identifier: 23994301
Funding acknowledgements
  • German Research Foundation: Hi 399/6-1
Open access
false
ISSN
0028-3908
Zeitschrift
Neuropharmacology
Schlüsselwörter
  • Brain
  • Cerebellum
  • Corpus Striatum
  • Animals
  • Mice, Knockout
  • Mice
  • Rats, Sprague-Dawley
  • Fluorine Radioisotopes
  • Benzamides
  • Cyclosporine
  • Enzyme Inhibitors
  • Radiopharmaceuticals
  • Positron-Emission Tomography
  • ATP Binding Cassette Transporter, Subfamily B
Sprache
eng
Medium
Print-Electronic
Online publication date
2013
Paginierung
152 - 158
Datum der Veröffentlichung
2014
Status
Published
Datum der Datenerfassung
2013
Titel
Evaluation of P-glycoprotein (abcb1a/b) modulation of [(18)F]fallypride in MicroPET imaging studies.
Sub types
  • Research Support, Non-U.S. Gov't
  • Journal Article
Ausgabe der Zeitschrift
84

Data source: Europe PubMed Central

Abstract
[(18)F]Fallypride ([(18)F]FP) is an important and routinely used D2/D3 antagonist for quantitative imaging of dopaminergic neurotransmission in vivo. Recently it was shown that the brain uptake of the structurally related [(11)C]raclopride is modulated by P-glycoprotein (P-gp), an important efflux transporter at the blood-brain barrier. The purpose of this study was to determine whether the brain uptake of [(18)F]FP is influenced by P-gp. For examination of this possible modulation microPET studies were performed in a rat and a mouse model. Hence, [(18)F]FP was applied to Sprague Dawley rats, half of them being treated with the P-gp inhibitor cyclosporine A (CsA). In a second experimental series the tracer was applied to three different groups of FVB/N mice: wild type, P-gp double knockout (abcb1a/1b (-/-)) and CsA-treated mice. In CsA-treated Sprague Dawley rats [(18)F]FP showed an elevated standard uptake value in the striatum compared to the control animals. In FVB/N mice a similar effect was observed, showing an increasing uptake from wild type to CsA-treated and double knockout mice. Since genetically or pharmacologically induced reduction of P-gp activity increased the uptake of [(18)F]FP markedly, we conclude that [(18)F]FP is indeed a substrate of P-gp and that the efflux pump modulates its brain uptake. This effect - if true for humans - may have particular impact on clinical studies using [(18)F]FP for assessment of D2/3 receptor occupancy by antipsychotic drugs. This article is part of the Special Issue Section entitled 'Neuroimaging in Neuropharmacology'.
Date of acceptance
2013
Autoren
  • Markus Piel
  • Ulrich Schmitt
  • Nicole Bausbacher
  • Hans-Georg Buchholz
  • Gerhard Gründer
  • Christoph Hiemke
  • Frank Rösch
Autoren-URL
https://www.ncbi.nlm.nih.gov/pubmed/23994301
DOI
10.1016/j.neuropharm.2013.04.062
eISSN
1873-7064
Zeitschrift
Neuropharmacology
Schlüsselwörter
  • Cyclosporine A
  • Dopamine D(2)/D(3) receptors
  • P-Glycoprotein
  • Positron emission tomography
  • [(18)F]fallypride
  • ATP Binding Cassette Transporter, Subfamily B
  • Animals
  • Benzamides
  • Brain
  • Cerebellum
  • Corpus Striatum
  • Cyclosporine
  • Enzyme Inhibitors
  • Fluorine Radioisotopes
  • Mice
  • Mice, Knockout
  • Positron-Emission Tomography
  • Radiopharmaceuticals
  • Rats, Sprague-Dawley
Sprache
eng
Country
England
Paginierung
152 - 158
PII
S0028-3908(13)00385-7
Datum der Veröffentlichung
2014
Status
Published
Datum, an dem der Datensatz öffentlich gemacht wurde
2015
Titel
Evaluation of P-glycoprotein (abcb1a/b) modulation of [(18)F]fallypride in MicroPET imaging studies.
Sub types
  • Journal Article
  • Research Support, Non-U.S. Gov't
Ausgabe der Zeitschrift
84

Data source: PubMed

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