gts 21

GTS-21 (DMXB-A) is an α7 nAChR agonist. GTS-21 suppresses inflammation associated with rheumatoid arthritis by inhibiting RA Th1 cell differentiation.

GTS-21 dihydrochloride (DMBX-anabaseine) is a nAChRs agonist. nAChRs are neuron receptor proteins that activated by the binding of the neurotransmitter ACh.

High affinity α7 nAChR partial agonist (Ki = 1.1 nM in rat; Emax < 10% of the response to ACh in rat and human). Inhibits ACh (IC50 = 2.7 nM) at α7 nAChR. Reduces LPS-induced TNF-α release from microglia enriched cultures. Anti-inflammatory. Briggs et al (2009) Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptors. Br.J.Pharmacol. 158 1486 PMID:19845675 |Thomsen et al (2012) The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia. J.Neuroimmunol. 251 65 PMID:22884467 |Papke et al (2015) The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor. Neuropharmacology 91 34 PMID:25497451