Nelonicline citrate  (Synonyms: ABT-126 citrate)

Nelonicline (ABT-126) citrate 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 citrate is used for the research of shizophrenia and Alzheimer's disease^[1][2][3].

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 (EC₅₀=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

505.54

C₂₃H₂₇N₃O₈S

1026136-84-4

O=C(O)CC(O)(CC(O)=O)C(O)=O.[C@@H]1([C@H]2C[C@H](C3)C[C@@H]1C[N@]3C2)OC4=NN=C(C5=CC=CC=C5)S4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhang D, et al. α7 nicotinic receptor agonists reduce levodopa-induced dyskinesias with severe nigrostriatal damage. Mov Disord. 2015;30(14):1901-1911.  [Content Brief]

  [2]. Haig G, et al. The α7 Nicotinic Agonist ABT-126 in the Treatment of Cognitive Impairment Associated with Schizophrenia in Nonsmokers: Results from a Randomized Controlled Phase 2b Study. Neuropsychopharmacology. 2016;41(12):2893-2902.  [Content Brief]

  [3]. Gault LM, et al. ABT-126 monotherapy in mild-to-moderate Alzheimer's dementia: randomized double-blind, placebo and active controlled adaptive trial and open-label extension. Alzheimers Res Ther. 2016;8(1):44. Published 2016 Oct 18.  [Content Brief]