Aryloxyethylamines: Binding at α7 nicotinic acetylcholine receptors

Structure–affinity relationships for the binding of 3-[2-(N,N,N-trimethylammonium)ethoxy]pyridine (AXPQ) at α7 nACh receptors were investigated due to its close structural similarity to a known α7 antagonist.

An examination of several aryloxyalkylamine analogs 4 and 5 was undertaken to determine the role of various structural features for binding at homomeric α7 nicotinic acetylcholine receptors. In general, the ring N atom might contribute to affinity but is not essential. In contrast, the N,N,N-trimethyl quaternary amine is a major contributor to α7 binding.Figure optionsDownload as PowerPoint slide