NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and bind with high affinity to heteromeric α3β4 and α4β2 nAChRs. NS3861 displays the β-subunit preference and a complete lack of activation at α4-containing receptors. The maximal efficacy of NS3861 appeared solely dependent on the nature of the ligand-binding domain. Furthermore, a principal subunit serine to threonine substitution may explain the lack of NS3861 activation at α4-containing receptors.

α4β4 (1:4):1.9 μm(Ki), α3β4:1 μm(Ki), α4β4 (4:1):1.2 μm(Ki), α3β2:1.6 μm(Ki)