Nelonicline citrate
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease.
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- CAS No.: 1026136-84-4
- Formule: C23H27N3O8S
- Masse moléculaire:505.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Nelonicline citrate 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 citrate 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 citrate 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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1026136-84-4
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Masse moléculaire 505.54
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Formule C23H27N3O8S
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SMILES
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
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Synonyms
ABT-126 citrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nelonicline citrate Related Classifications
HY-16748A Related Classifications
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