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High-affinity Fluorescent Ligands for the 5-HT3 Receptor

Type of publication Peer-reviewed
Publikationsform Original article (peer-reviewed)
Publication date 2011
Author Simonin Jonathan, Vernekar Sanjeev Kumar V., Thompson Andrew J., Hothersall Daniel J., Connolly Christopher N., Lummis Sarah C. R., Lochner Martin,
Project Synthetic Neurochemistry - Introduction of Biophysical Tools into Ion Channels Using Chemical Approaches
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Original article (peer-reviewed)

Journal Bioorganic & Medicinal Chemistry Letters
Volume (Issue) 22(2)
Page(s) 1151 - 1155
Title of proceedings Bioorganic & Medicinal Chemistry Letters
DOI 10.1016/j.bmcl.2011.11.097


The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT3AR.