sax 3

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 (SAX-187) 是一种有效的选择性5-HT6受体激动剂，Ki 为 2.2 nM，EC50为 6.6 nM。它介导 5-HT6 受体依赖性信号通路，可作为特异性激动剂。

WAY-181187 (SAX-187) oxalate 是一种选择性的、有效的 5-HT6 受体的激动剂 (Ki: 2.2 nM; EC50: 6.6 nM)。WAY-181187 oxalate 是一种特异性激动剂，介导 5-HT6 受体依赖性信号通路（如 cAMP，Fyn 和 ERK1/2 激酶）。