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Synonyms: AQW-051 | VQW 765 | VQW-765 | VQW765
Compound class: Synthetic organic
Comment: AQW 051 is an α7 nicotinic acetylcholine receptor (nAChR) partial agonist from Novartis for the oral treatment of cognitive deficits in schizophrenia, Alzheimer's, and Parkinson's diseases [1,3]. Structure first disclosed at March 2014 ACS meeting. The (3S) version is CID 71553840. The compound was later re-named to VQW-765 (Vanda Pharmaceuticals).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Di Paolo T, Grégoire L, Feuerbach D, Elbast W, Weiss M, Gomez-Mancilla B. (2014)
AQW051, a novel and selective nicotinic acetylcholine receptor α7 partial agonist, reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys.
Parkinsonism Relat Disord, 20 (11): 1119-23. [PMID:25172125]
2. Di Paolo, Thérèse et. al. (2011)
Use of nicotinic acetylcholine receptor alpha 7 activators.
Patent number: WO2011036167. Assignee: Novartis. Priority date: 22/09/2009. Publication date: 31/03/2011.
3. Feuerbach D, Pezous N, Weiss M, Shakeri-Nejad K, Lingenhoehl K, Hoyer D, Hurth K, Bilbe G, Pryce CR, McAllister K et al.. (2015)
AQW051, a novel, potent and selective α7 nicotinic ACh receptor partial agonist: pharmacological characterization and phase I evaluation.
Br J Pharmacol, 172 (5): 1292-304. [PMID:25363835]
4. Hurth K, et. al.
MEDI 222: Identification of AQW051, an alpha7 nicotinic acetylcholine receptor partial agonist for the treatment of cognitive impairment associated with schizophrenia.
Accessed on 06/04/2014. Modified on 06/04/2014. ACS Med Chem Meeting Abstracts, March 2014, http://www.acsmedchem.org/mediabstracts2014.pdf
5. Trenkwalder C, Berg D, Rascol O, Eggert K, Ceballos-Baumann A, Corvol JC, Storch A, Zhang L, Azulay JP, Broussolle E et al.. (2016)
A Placebo-Controlled Trial of AQW051 in Patients With Moderate to Severe Levodopa-Induced Dyskinesia.
Mov Disord, 31 (7): 1049-54. [PMID:26990766]