[C]4-甲氧基-[2-(噻吩-2-基)咪唑并[1,2-a]吡啶-3-基]苯甲酰胺作为一种对含δ亚基的A型γ-氨基丁酸受体具有选择性的脑渗透性正电子发射断层显像（PET）配体的合成及药理评价
Synthesis and Pharmacological Evaluation of [C]4-Methoxy--[2-(thiophen-2-yl)imidazo[1,2-]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors.
作者信息
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
机构信息
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
Neurobiology Research Unit and CIMBI, Copenhagen University Hospital, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark.
出版信息
ACS Omega. 2019 May 22;4(5):8846-8851. doi: 10.1021/acsomega.9b00434. eCollection 2019 May 31.
The αβδ-containing GABA 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 () as a candidate radiotracer, C-labeling, and subsequent evaluation of [C]DS2OMe in a domestic pig as a PET radioligand for visualization of the δ-containing GABA receptors.
含αβδ的GABA受体与多种脑部疾病有关。尽管有开发δ选择性成像剂的潜力，但目前尚无用于体内成像的PET放射性配体。在此，我们报告了DS2OMe（）作为候选放射性示踪剂的特性、碳标记，以及随后在国内猪体内对[碳]DS2OMe作为PET放射性配体用于可视化含δ的GABA受体的评估。
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