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Synonyms: A-793394 | A793394 | NS-6740
Compound class: Synthetic organic
Comment: NS6740 (A-582941) is described as a silent agonist (or metagonist) of α7 nicotinic acetylcholine receptors (CHRNA7; nAChR, a ligand-gated ion channel) . This means that it binds to the receptor but has no intrinsic agonist activity (and may induce conformational change to a non-conducting state), but it does increase receptor sensitivity to positive allosteric modulators (PAMs). The α7 nAChR; is a promising drug target inflammatory diseases and neurological disorders (e.g. chronic and neuropathic) pain. NS6740 can be used to explore the most suitable mechanistic approach by which to achive clinical benefit from modulating the α7 nAChR .
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. Briggs CA, Grønlien JH, Curzon P, Timmermann DB, Ween H, Thorin-Hagene K, Kerr P, Anderson DJ, Malysz J, Dyhring T et al.. (2009)
Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptors.
Br J Pharmacol, 158 (6): 1486-94. [PMID:19845675]
2. Papke RL, Bagdas D, Kulkarni AR, Gould T, AlSharari SD, Thakur GA, Damaj MI. (2015)
The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor.
Neuropharmacology, 91: 34-42. [PMID:25497451]