NS3861

Description: NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) that binds with high affinity to heteromeric alpha3beta4 and alpha4beta2 nAChRs, displaying beta-subunit preference and no activation at alpha4-containing receptors. The maximal efficacy of NS3861 depends on the ligand-binding domain, and a serine to threonine substitution in the principal subunit may explain the lack of activation at alpha4-containing receptors. Target: AChR. Smiles: CN1C2CCC1C=C(C2)c1sccc1Br. References: Harpsøe K et al. Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors. J Biol Chem. 2013 Jan 25,288(4):2559-70.