sax 187

SAX-187 (SAX-187) has high-affinity binding at the human 5-HT6 receptor.

SAX-187 hydrochloride is a potent and selective 5-HT6 receptor agonist. SAX-187 hydrochloride possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (SAX-187 hydrochloride: EC50=6.6 nM, Emax=93%). In the rat frontal cortex, acute administration of SAX-187 hydrochloride (3-30 mg/kg, subcutaneous (s.c.)) significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine.

WAY-181187 (SAX-187) oxalate is a selective and potent agonist of the 5-HT6 receptor (Ki: 2.2 nM; EC50: 6.6 nM) that mediates 5-HT6 receptor-dependent signaling pathways, including cAMP, Fyn, and ERK1/2 kinases.