Nelonicline

Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (K_i=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease^[1][2][3]. IC50 & Target: Neuronal nicotinic receptor^[1] In Vitro: Nelonicline is an agonist that binds with high affinity to α7 nAChRs in human brain (K_i= 12.3 nM) and activates currents in Xenopus oocytes expressing recombinant human α7 nAChRs (EC₅₀=2 μM; intrinsic activity of 74% relative to acetylcholine). Nelonicline does bind to α3β4* nAChRs in human IMR-32 neuroblastoma cells (K_i=60 nM), but has only 12% efficacy at 100,000 nM in a calcium flux assay in these cell. Like some other α7 nAChR agonists, Nelonicline is also a 5-HT3 receptor antagonist, but it has >10-fold lower affinity for this receptor than for α7 nAChRs (K_i of 140 nM)^[1].