Nelonicline citrate (ABT-126) is an orally active and selective α7 nicotinic receptor agonist, demonstrating a high affinity for α7 nAChRs in the human brain (Ki = 12.3 nM). This compound is utilized in the research of schizophrenia and Alzheimer's disease.

Nelonicline citrate 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 (EC 50 =2 μM; intrinsic activity of 74% relative to acetylcholine). Nelonicline citrate 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 citrate 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].