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

NS3861被发现能激活野生型α3β4 nAChRs（见图3R和图4），但并未能激活野生型α4β2。NS3861在α3β4上表现为部分激动剂，然而在α3β2上则为全激动剂，尽管其效力约为结合亲和力的十分之一。在α3/α4 + β4/β2受体上的效能几乎与野生型α3β4相同，而在α4/α3 + β2/β4上未见效能[1]。