Abstract
3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. Diverse spacer motifs were incorporated between the hydrogen bond acceptor (HBA) part and a variety of substituted (hetero)aryl moieties. Bispidine carboxamides bearing spacer motifs often showed high affinity in the low nanomolar range and selectivity for the α4β2∗ nAChR. Compounds 15, 25, and 47 with Ki values of about 1nM displayed the highest affinities for α4β2∗ nAChR. All evaluated compounds are partial agonists or antagonists at α4β2∗, with reduced or no effects on α3β4∗ with the exception of compound 15 (agonist), and reduced or no effect at α7 and muscle subtypes.
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