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Synthesis and Characterization of Photoaffinity Probes that Target the 5-HT3 Receptor

Type of publication Not peer-reviewed
Publikationsform Original article (non peer-reviewed)
Publication date 2014
Author Jack Thomas, Ruepp Marc-David, Thompson Andrew J., Mühlemann Oliver, Lochner Martin (corresponding author),
Project Synthetic Neurochemistry - Introduction of Biophysical Tools into Ion Channels Using Chemical Approaches
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Original article (non peer-reviewed)

Journal Chimia
Volume (Issue) 68(4)
Page(s) 239 - 242
Title of proceedings Chimia
DOI 10.2533/chimia.2014.239


The 5-HT3 receptor is one of several ion channels responsible for the transmission of nerve impulses in the peripheral and central nervous systems. Until now, it has been difficult to characterize transmembrane receptors with classical structural biology approaches like X-ray crystallography. The use of photoaffinity probes is an alternative approach to identify regions in the protein where small molecules bind. To this end, we present two photoaffinity probes based on granisetron, a well known antagonist of the 5-HT3 receptor. These new probes show nanomolar binding affinity for the orthosteric binding site. In addition, we investigated their reactivity using irradiation experiments.