Synthesis and Pharmacological Evaluation of [11C] 4-Methoxy-N-[2-(thiophen-2-yl) imidazo [1, 2-a] pyridin-3-yl] benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors
- Publikationstyp:
- Zeitschriftenaufsatz
- Metadaten:
-
- Autoren
- Elina T L'Estrade
- Hanne D Hansen
- Christina Falk-Petersen
- Anne Haugaard
- Nane Griem-Krey
- Sascha Jung
- Hartmut Lueddens
- Tanja Schirmeister
- Maria Erlandsson
- Tomas Ohlsson
- Gitte M Knudsen
- Matthias M Herth
- Petrine Wellendorph
- Bente Frolund
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000470094000106&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.1021/acsomega.9b00434
- Externe Identifier
- Clarivate Analytics Document Solution ID: IB2IX
- PubMed Identifier: 31459972
- ISSN
- 2470-1343
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- ACS OMEGA
- Paginierung
- 8846 - 8851
- Datum der Veröffentlichung
- 2019
- Status
- Published
- Titel
- Synthesis and Pharmacological Evaluation of [<SUP>11</SUP>C]4-Methoxy-<i>N</i>-[2-(thiophen-2-yl) imidazo[1,2-<i>a</i>] pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors
- Sub types
- Article
- Ausgabe der Zeitschrift
- 4
Datenquelle: Web of Science (Lite)
- Andere Metadatenquellen:
-
- Autoren
- Elina T L’Estrade
- Hanne D Hansen
- Christina Falk-Petersen
- Anne Haugaard
- Nane Griem-Krey
- Sascha Jung
- Hartmut Lüddens
- Tanja Schirmeister
- Maria Erlandsson
- Tomas Ohlsson
- Gitte M Knudsen
- Matthias M Herth
- Petrine Wellendorph
- Bente Frølund
- DOI
- 10.1021/acsomega.9b00434
- eISSN
- 2470-1343
- ISSN
- 2470-1343
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- ACS Omega
- Sprache
- en
- Online publication date
- 2019
- Paginierung
- 8846 - 8851
- Datum der Veröffentlichung
- 2019
- Status
- Published
- Herausgeber
- American Chemical Society (ACS)
- Herausgeber URL
- http://dx.doi.org/10.1021/acsomega.9b00434
- Datum der Datenerfassung
- 2023
- Titel
- Synthesis and Pharmacological Evaluation of [<sup>11</sup>C]4-Methoxy-<i>N</i>-[2-(thiophen-2-yl)imidazo[1,2-<i>a</i>]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors
- Ausgabe der Zeitschrift
- 4
Datenquelle: Crossref
- Abstract
- The α<sub>4/6</sub>βδ-containing GABA<sub>A</sub> receptors are involved in a number of brain diseases. Despite the potential of a δ-selective imaging agent, no PET radioligand is currently available for in vivo imaging. Here, we report the characterization of DS2OMe (<b>1</b>) as a candidate radiotracer, <sup>11</sup>C-labeling, and subsequent evaluation of [<sup>11</sup>C]DS2OMe in a domestic pig as a PET radioligand for visualization of the δ-containing GABA<sub>A</sub> receptors.
- Addresses
- Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
- Autoren
- Elina T L'Estrade
- Hanne D Hansen
- Christina Falk-Petersen
- Anne Haugaard
- Nane Griem-Krey
- Sascha Jung
- Hartmut Lüddens
- Tanja Schirmeister
- Maria Erlandsson
- Tomas Ohlsson
- Gitte M Knudsen
- Matthias M Herth
- Petrine Wellendorph
- Bente Frølund
- DOI
- 10.1021/acsomega.9b00434
- eISSN
- 2470-1343
- Externe Identifier
- PubMed Identifier: 31459972
- PubMed Central ID: PMC6648289
- Funding acknowledgements
- Lundbeck Foundation: R164-2013-15384
- Lundbeck Foundation: R230-2016-2562
- Lundbeck Foundation: R139-2012-12270
- Open access
- true
- ISSN
- 2470-1343
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- ACS omega
- Sprache
- eng
- Medium
- Electronic-eCollection
- Online publication date
- 2019
- Open access status
- Open Access
- Paginierung
- 8846 - 8851
- Datum der Veröffentlichung
- 2019
- Status
- Published
- Datum der Datenerfassung
- 2019
- Titel
- Synthesis and Pharmacological Evaluation of [<sup>11</sup>C]4-Methoxy-<i>N</i>-[2-(thiophen-2-yl)imidazo[1,2-<i>a</i>]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors.
- Sub types
- research-article
- Journal Article
- Ausgabe der Zeitschrift
- 4
Files
https://pubs.acs.org/doi/pdf/10.1021/acsomega.9b00434 https://europepmc.org/articles/PMC6648289?pdf=render
Datenquelle: Europe PubMed Central
- Abstract
- The α4/6βδ-containing GABAA receptors are involved in a number of brain diseases. Despite the potential of a δ-selective imaging agent, no PET radioligand is currently available for in vivo imaging. Here, we report the characterization of DS2OMe (1) as a candidate radiotracer, 11C-labeling, and subsequent evaluation of [11C]DS2OMe in a domestic pig as a PET radioligand for visualization of the δ-containing GABAA receptors.
- Date of acceptance
- 2019
- Autoren
- Elina T L'Estrade
- Hanne D Hansen
- Christina Falk-Petersen
- Anne Haugaard
- Nane Griem-Krey
- Sascha Jung
- Hartmut Lüddens
- Tanja Schirmeister
- Maria Erlandsson
- Tomas Ohlsson
- Gitte M Knudsen
- Matthias M Herth
- Petrine Wellendorph
- Bente Frølund
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/31459972
- DOI
- 10.1021/acsomega.9b00434
- eISSN
- 2470-1343
- Externe Identifier
- PubMed Central ID: PMC6648289
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- ACS Omega
- Sprache
- eng
- Country
- United States
- Paginierung
- 8846 - 8851
- Datum der Veröffentlichung
- 2019
- Status
- Published online
- Titel
- Synthesis and Pharmacological Evaluation of [11C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors.
- Sub types
- Journal Article
- Ausgabe der Zeitschrift
- 4
Datenquelle: PubMed
- Autoren
- Elina T L’Estrade
- Hanne D Hansen
- Christina Falk-Petersen
- Anne Haugaard
- Nane Griem-Krey
- Sascha Jung
- Hartmut Lüddens
- Tanja Schirmeister
- Maria Erlandsson
- Tomas Ohlsson
- others
- Zeitschrift
- ACS Omega
- Artikelnummer
- 5
- Paginierung
- 8846 - 8851
- Datum der Veröffentlichung
- 2019
- Herausgeber
- ACS Publications
- Datum der Datenerfassung
- 2021
- Titel
- Synthesis and Pharmacological Evaluation of [11C] 4-Methoxy-N-[2-(thiophen-2-yl) imidazo [1, 2-a] pyridin-3-yl] benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors
- Sub types
- article
- Ausgabe der Zeitschrift
- 4
Datenquelle: Manual
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