Nelonicline (ABT-126) 是一种有效、选择性的 α7 烟碱受体 (α7 nAChR) 激动剂，在人脑中与α7 nAChRs 具有高度亲和力 (K_i=12.3 nM)。Nelonicline 用于精神分裂症和阿尔茨海默病的研究。

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 Alzheimers disease.

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Neuronal nicotinic receptor

Nelonicline is an agonist that binds with high affinity to α7 nAChRs in human brain (Ki= 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 (Ki=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 (Ki of 140 nM). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

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

In Vitro: DMSO : 12.5 mg/mL (39.88 mM; ultrasonic and warming and heat to 60°C)配制储备液