High-affinity fluorescent ligands for the 5-HT 3 receptor

Jonathan Simonin, Sanjeev Kumar V. Vernekar, Andrew J. Thompson, J. Daniel Hothersall, Christopher N. Connolly, Sarah C.R. Lummis, Martin Lochner

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13 Scopus citations

Abstract

The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT 3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT 3AR.

Original languageEnglish (US)
Pages (from-to)1151-1155
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number2
DOIs
StatePublished - Jan 15 2012

Bibliographical note

Funding Information:
This research was supported by the Swiss National Science Foundation (SNSF-professorship PP00P2_123536 to ML), the EPSRC (EP/E042139/1) and the Wellcome Trust (085141 (CNC and JDH) and 081925/Z/07/Z (SCRL and AJT)). SCRL is a Wellcome Trust Senior Research Fellow in Basic Biomedical Science.

Copyright:
Copyright 2012 Elsevier B.V., All rights reserved.

Keywords

  • 5-HT receptor
  • Cys-loop ligand-gated ion channels
  • Fluorescent ligands
  • In vivo imaging
  • Radioligand binding

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