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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

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, etc.

ACS Omega. 2019 May 22;4(5):8846-8851.

PMID: 31459972

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
LS7931260 Imidazo[1,2-a]pyridine-6-boronic acid Imidazo[1,2-a]pyridine-6-boronic acid Price
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