WAY-181187 (oxalate)

WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a K_i of 2.2 nM and an EC₅₀ of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist^[1][2]. In Vitro:WAY-181187 (SAX-187) oxalate (1 and 10 μM) increases activation of ERK1/2. WAY181187 also increases Fyn kinase activity^[2]. In Vivo:Acute administration of WAY-181187 (SAX-187) oxalate (3-30 mg/kg, s.c.) significantly increases extracellular GABA concentrations without altering the levels of glutamate or norepinephrine in the rat frontal cortex. Additionally, WAY-181187 oxalate (30 mg/kg, s.c.) produces modest yet significant decreases in cortical dopamine and 5-HT levels^[1].