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

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.

OriginalsprogEngelsk
TidsskriftACS omega
Vol/bind4
Udgave nummer5
Sider (fra-til)8846-8851
Antal sider6
ISSN2470-1343
DOI
StatusUdgivet - 31 maj 2019

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