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Updated: Aug 21, 2026

Localization of Plasma Membrane and Intracellular Neuronal Nicotinic Acetylcholine Receptors Using Quantitative Imaging in Mammalian Cells
Published on: December 19, 2025
Norchloro-fluoro-homoepibatidine: specificity to neuronal nicotinic acetylcholine receptor subtypes in vitro
Winnie Deuther-Conrad1, Jörg Thomas Patt, Dominik Feuerbach
1Institute of Interdisciplinary Isotope Research, Permoserstrasse 15, D-04318, Leipzig, Germany. conrad@iif-leipzig.de
Abstract:
The subtype-specificity of newly synthesised epibatidine-related compounds, norchloro-fluoro-homoepibatidine (NCFHEB) and derivatives, to neuronal nicotinic acetylcholine receptors (nAChR) has been investigated. NCFHEBs were assayed in competitive binding assays to (+/-)-[(3)H]epibatidine-labelled rat thalamic nAChRs and human alpha4beta2, alpha3beta4, and alpha7 nAChRs, expressed in stably transfected HEK-293 and SH-SY5Y cells. The binding affinity of (+)-NCFHEB (K(i): 0.064 nM) and (-)-NCFHEB (K(i): 0.112 nM) to human alpha4beta2 nAChR is in the same order of magnitude as that of epibatidine (K(i): 0.014 nM). However, because the affinity of both NCFHEB-enantiomers to human alpha3beta4 nAChR is up to 65 times lower than that of epibatidine, the alpha4beta2 subtype-specificity of NCFHEB is increased up to 1,400% compared to epibatidine.
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