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Synthesis and Pharmacological Evaluation of [(11)C]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
[Image: see text] The α(4/6)βδ-containing GABA(A) 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,...
| Autores principales: | , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2019
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6648289/ https://www.ncbi.nlm.nih.gov/pubmed/31459972 http://dx.doi.org/10.1021/acsomega.9b00434 |
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| author | L’Estrade, Elina T. Hansen, Hanne D. Falk-Petersen, Christina Haugaard, Anne Griem-Krey, Nane Jung, Sascha Lüddens, Hartmut Schirmeister, Tanja Erlandsson, Maria Ohlsson, Tomas Knudsen, Gitte M. Herth, Matthias M. Wellendorph, Petrine Frølund, Bente |
| author_facet | L’Estrade, Elina T. Hansen, Hanne D. Falk-Petersen, Christina Haugaard, Anne Griem-Krey, Nane Jung, Sascha Lüddens, Hartmut Schirmeister, Tanja Erlandsson, Maria Ohlsson, Tomas Knudsen, Gitte M. Herth, Matthias M. Wellendorph, Petrine Frølund, Bente |
| author_sort | L’Estrade, Elina T. |
| collection | PubMed |
| description | [Image: see text] The α(4/6)βδ-containing GABA(A) 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, (11)C-labeling, and subsequent evaluation of [(11)C]DS2OMe in a domestic pig as a PET radioligand for visualization of the δ-containing GABA(A) receptors. |
| format | Online Article Text |
| id | pubmed-6648289 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2019 |
| publisher | American Chemical Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-66482892019-08-27 Synthesis and Pharmacological Evaluation of [(11)C]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 L’Estrade, Elina T. Hansen, Hanne D. Falk-Petersen, Christina Haugaard, Anne Griem-Krey, Nane Jung, Sascha Lüddens, Hartmut Schirmeister, Tanja Erlandsson, Maria Ohlsson, Tomas Knudsen, Gitte M. Herth, Matthias M. Wellendorph, Petrine Frølund, Bente ACS Omega [Image: see text] The α(4/6)βδ-containing GABA(A) 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, (11)C-labeling, and subsequent evaluation of [(11)C]DS2OMe in a domestic pig as a PET radioligand for visualization of the δ-containing GABA(A) receptors. American Chemical Society 2019-05-22 /pmc/articles/PMC6648289/ /pubmed/31459972 http://dx.doi.org/10.1021/acsomega.9b00434 Text en Copyright © 2019 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
| spellingShingle | L’Estrade, Elina T. Hansen, Hanne D. Falk-Petersen, Christina Haugaard, Anne Griem-Krey, Nane Jung, Sascha Lüddens, Hartmut Schirmeister, Tanja Erlandsson, Maria Ohlsson, Tomas Knudsen, Gitte M. Herth, Matthias M. Wellendorph, Petrine Frølund, Bente Synthesis and Pharmacological Evaluation of [(11)C]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 |
| title | Synthesis and Pharmacological Evaluation of [(11)C]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 |
| title_full | Synthesis and Pharmacological Evaluation of [(11)C]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 |
| title_fullStr | Synthesis and Pharmacological Evaluation of [(11)C]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 |
| title_full_unstemmed | Synthesis and Pharmacological Evaluation of [(11)C]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 |
| title_short | Synthesis and Pharmacological Evaluation of [(11)C]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 |
| title_sort | synthesis and pharmacological evaluation of [(11)c]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 |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6648289/ https://www.ncbi.nlm.nih.gov/pubmed/31459972 http://dx.doi.org/10.1021/acsomega.9b00434 |
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