676524-06-4Relevant academic research and scientific papers
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A1Receptor in Living Cells
Comeo, Eleonora,Trinh, Phuc,Nguyen, Anh T.,Nowell, Cameron J.,Kindon, Nicholas D.,Soave, Mark,Stoddart, Leigh A.,White, Jonathan M.,Hill, Stephen J.,Kellam, Barrie,Halls, Michelle L.,May, Lauren T.,Scammells, Peter J.
, p. 6670 - 6695 (2021)
The adenosine A1 receptor (A1AR) is a G-protein-coupled receptor (GPCR) that provides important therapeutic opportunities for a number of conditions including congestive heart failure, tachycardia, and neuropathic pain. The development of A1AR-selective fluorescent ligands will enhance our understanding of the subcellular mechanisms underlying A1AR pharmacology facilitating the development of more efficacious and selective therapies. Herein, we report the design, synthesis, and application of a novel series of A1AR-selective fluorescent probes based on 8-functionalized bicyclo[2.2.2]octylxanthine and 3-functionalized 8-(adamant-1-yl) xanthine scaffolds. These fluorescent conjugates allowed quantification of kinetic and equilibrium ligand binding parameters using NanoBRET and visualization of specific receptor distribution patterns in living cells by confocal imaging and total internal reflection fluorescence (TIRF) microscopy. As such, the novel A1AR-selective fluorescent antagonists described herein can be applied in conjunction with a series of fluorescence-based techniques to foster understanding of A1AR molecular pharmacology and signaling in living cells.
Novel aromatic compounds possessing antifungal or antibacterial activity
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Page/Page column 39; 59; 60, (2010/02/06)
The present invention provides novel compounds possessing antibacterial, antifungal, antiviral, anticancer, and/or antiparasitic activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds ar
