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Fluorescent Agonists of the α7 Nicotinic Acetylcholine Receptor Derived from 3‐Amino‐Quinuclidine

Type of publication Peer-reviewed
Publikationsform Original article (peer-reviewed)
Author Bürgi Justus J., Bertrand Sonia, Marger Fabrice, Bertrand Daniel, Reymond Jean-Louis,
Project Exploiting and Extending GDB for Drug Discovery
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Original article (peer-reviewed)

Journal Helvetiac Chimia Acta
Volume (Issue) 99
Page(s) 790 - 804
Title of proceedings Helvetiac Chimia Acta
DOI 10.1002/hlca.201600120

Open Access

Abstract

Here, we investigated whether fluorescence labeled small molecule agonists of the α7 nicotinic acetylcholine receptor (nAChR) might be identified to enhance receptor studies. Enantiomerically pure 3‐amino‐quinuclidines appended with fluorophores at the 3‐amino group were synthesized and tested by electrophysiology on human α7 nAChR in Xenopus oocytes, uncovering (R)‐4 and (R)‐9 as the first examples of fluorescent α7 nAChR agonists. These molecules elegantly incorporate the fluorescent reporter group as part of the pharmacophore itself and provide a new class of tool compounds for the study of these ligand‐gated ion channels.
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