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Updated: Apr 18, 2026
High-resolution Spatiotemporal Analysis of Receptor Dynamics by Single-molecule Fluorescence Microscopy
Published on: July 25, 2014
Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved
Iuliia A Karpenko1, Jean-François Margathe, Thiéric Rodriguez
1Laboratoire d'Innovation Thérapeutique, UMR7200 CNRS/Université de Strasbourg, Labex MEDALIS, Faculté de Pharmacie , 74 route du Rhin, 67401 Illkirch, France.
Abstract:
The design and the synthesis of the first high-affinity fluorescent ligands for oxytocin receptor (OTR) are described. These compounds enabled the development of a TR-FRET based assay for OTR, readily amenable to high throughput screening. The validation of the assay was achieved by competition experiments with both peptide and nonpeptide OTR ligands as competitors. These probes represent the first selective fluorescent ligands for the oxytocin G protein-coupled receptor.
