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.

Authors :: 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
Source :: ACS omega [ACS Omega] 2019 May 22; Vol. 4 (5), pp. 8846-8851. Date of Electronic Publication: 2019 May 22 (Print Publication: 2019).
Publication Year :: 2019
Abstract: The α <subscript>4/6</subscript> βδ-containing GABA <subscript>A</subscript> 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, <superscript>11</superscript> C-labeling, and subsequent evaluation of [ <superscript>11</superscript> C]DS2OMe in a domestic pig as a PET radioligand for visualization of the δ-containing GABA <subscript>A</subscript> receptors.<br />Competing Interests: The authors declare no competing financial interest.

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