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

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

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

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

Abstrakt

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.

Originalsprog	Engelsk
Tidsskrift	ACS omega
Vol/bind	4
Udgave nummer	5
Sider (fra-til)	8846-8851
Antal sider	6
ISSN	2470-1343
DOI	https://doi.org/10.1021/acsomega.9b00434
Status	Udgivet - 31 maj 2019

Adgang til dokumentet

10.1021/acsomega.9b00434

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Citationsformater

L'Estrade, E. T., Hansen, H. D., Falk-Petersen, C., Haugaard, A., Griem-Krey, N., Jung, S., Lüddens, H., Schirmeister, T., Erlandsson, M., Ohlsson, T., Knudsen, G. M., Herth, M. M., Wellendorph, P., & Frølund, B. (2019). 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. ACS omega, 4(5), 8846-8851. https://doi.org/10.1021/acsomega.9b00434

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. / L'Estrade, Elina T; Hansen, Hanne D; Falk-Petersen, Christina et al.

I: ACS omega, Bind 4, Nr. 5, 31.05.2019, s. 8846-8851.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

L'Estrade, ET, Hansen, HD, Falk-Petersen, C, Haugaard, A, Griem-Krey, N, Jung, S, Lüddens, H, Schirmeister, T, Erlandsson, M, Ohlsson, T, Knudsen, GM , Herth, MM, Wellendorph, P & Frølund, B 2019, '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', ACS omega, bind 4, nr. 5, s. 8846-8851. https://doi.org/10.1021/acsomega.9b00434

L'Estrade ET, Hansen HD, Falk-Petersen C, Haugaard A, Griem-Krey N, Jung S et al. 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. ACS omega. 2019 maj 31;4(5):8846-8851. https://doi.org/10.1021/acsomega.9b00434

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title = "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",

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.",

author = "L'Estrade, {Elina T} and Hansen, {Hanne D} and Christina Falk-Petersen and Anne Haugaard and Nane Griem-Krey and Sascha Jung and Hartmut L{\"u}ddens and Tanja Schirmeister and Maria Erlandsson and Tomas Ohlsson and Knudsen, {Gitte M} and Herth, {Matthias M} and Petrine Wellendorph and Bente Fr{\o}lund",

year = "2019",

month = may,

day = "31",

doi = "10.1021/acsomega.9b00434",

language = "English",

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AU - L'Estrade, Elina T

AU - Hansen, Hanne D

AU - Falk-Petersen, Christina

AU - Haugaard, Anne

AU - Griem-Krey, Nane

AU - Jung, Sascha

AU - Lüddens, Hartmut

AU - Schirmeister, Tanja

AU - Erlandsson, Maria

AU - Ohlsson, Tomas

AU - Knudsen, Gitte M

AU - Herth, Matthias M

AU - Wellendorph, Petrine

AU - Frølund, Bente

PY - 2019/5/31

Y1 - 2019/5/31

N2 - 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.

AB - 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.

U2 - 10.1021/acsomega.9b00434

DO - 10.1021/acsomega.9b00434

M3 - Journal article

C2 - 31459972

VL - 4

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JO - ACS Omega

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SN - 2470-1343

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