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Purity: ≥98%
Nelonicline (aslo known as ABT-126) is a novel, potent and selective neuronal nicotinic receptor agonist. Nelonicline is potentially useful for the treatment of Alzheimer's diseases. ABT-126 may be useful to reduce dyskinesias in both early- and later-stage Parkinson's disease. Accumulating evidence suggests that the α7 subtype of nicotinic acetylcholine receptors (nAChRs) plays a key role in inflammatory processes, thought to be involved in the pathophysiology of neuropsychiatric diseases, such as schizophrenia and Alzheimer's disease.
| ln Vitro |
Nelonicline is an agonist that exhibits a high affinity (Ki = 12.3 nM) for human brain α7 nAChR. It also causes currents to be activated in Xenopus laevis oocytes that express recombinant human α7 nAChR (EC50 = 2 μM; 74% intrinsic activity in relation to acetylcholine). In human IMR-32 neuroblastoma cells, neronicline does bind to α3β4* nAChR (Ki=60 nM); however, in calcium flux tests in these cells, it is only 12% effective at 100,000 nM. Nelonicline is a 5-HT3 receptor antagonist, just like some other α7 nAChR agonists, however its affinity for this receptor is more than ten times lower than that of α7 nAChR (Ki of 140 nM) [1].
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| References |
[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. [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 |
| Molecular Formula |
C17H19N3OS
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|---|---|
| Molecular Weight |
313.41726231575
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| CAS # |
1026134-63-3
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| SMILES |
C1(C(S2)=NN=C2O[C@@H]3[C@H]4C[C@H]5C[C@@H]3CN(C4)C5)=CC=CC=C1
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| InChi Key |
QZDCYUCETTWCMO-OFTMQHFLSA-N
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| InChi Code |
InChI=1S/C17H19N3OS/c1-2-4-12(5-3-1)16-18-19-17(22-16)21-15-13-6-11-7-14(15)10-20(8-11)9-13/h1-5,11,13-15H,6-10H2/t11-,13-,14+,15+
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| Chemical Name |
2-(((3R,4r,5S,7s)-1-azaadamantan-4-yl)oxy)-5-phenyl-1,3,4-thiadiazole
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| Synonyms |
ABT-126; ABT126; ABT 126
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~39.88 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1906 mL | 15.9530 mL | 31.9061 mL | |
| 5 mM | 0.6381 mL | 3.1906 mL | 6.3812 mL | |
| 10 mM | 0.3191 mL | 1.5953 mL | 3.1906 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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