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.
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.
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.
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