753500-02-6
Chemical Structure
NS-6740
- CAS No.: 753500-02-6
- Formula:C19H19F3N2O2
- Molecular Weight:364.36
IUPAC Name: (1,4-diazabicyclo[3.2.2]nonan-4-yl)(5-(3-(trifluoromethyl)phenyl)furan-2-yl)methanone
InChIKey: VSOWCIMCDKXVRC-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(O1)C2=CC=CC(C(F)(F)F)=C2)N3CCN4CCC3CC4
Biological Activity: NS-6740 is a partial agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 also acts as a potent modulator of the cholinergic anti-inflammatory pathway. NS-6740 alters the signaling pattern of α7 in an ion channel-independent manner, thereby reducing synaptic function. NS-6740 induces the desensitized state of α7 nAChR. NS-6740 generates robust nAChR-mediated currents. NS-6740 reduces LPS (HY-D1056)-induced TNF-α release from microglia. NS-6740 can be used in the research of neuroinflammation and neuropathic pain[1][2].
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NS-6740 | NS-6740 is a partial agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 also acts as a potent modulator of the cholinergic anti-inflammatory pathway. NS-6740 alters the signaling pattern of α7 in an ion channel-independent manner, thereby reducing synaptic function. NS-6740 induces the desensitized state of α7 nAChR. NS-6740 generates robust nAChR-mediated currents. NS-6740 reduces LPS (HY-D1056)-induced TNF-α release from microglia. NS-6740 can be used in the research of neuroinflammation and neuropathic pain. | |||||||||||||||||||||
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- [1]. Thomsen MS, et al., The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia. J Neuroimmunol. 2012 Oct 15;251(1-2):65-72. [Content Brief]
- [2]. Papke RL, et al., NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity. Neurosci Lett. 2018 Jun 11;677:6-13. [Content Brief]
Keywords
