NS3861 is a high-affinity agonist selectively targeting heteromeric alpha3beta4 and alpha4beta2 nicotinic acetylcholine receptors, yet it uniquely fails to activate alpha4-containing subtypes. This functional selectivity, influenced by specific beta-subunits and a key serine residue, makes it a valuable research tool for studying nAChR pharmacology and neurobiology in both in vitro and in vivo models.