SAX-187 hydrochloride

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.