way-181187

Description: WAY-181187 (SAX187) is a novel, potent and selective 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (WAY- EC50=6.6 nM, Emax=93%). In the rat frontal cortex, acute administration of WAY-181187 (3-30 mg/kg, subcutaneous (s.c.)) significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine.

References: Brouard JT, Schweimer JV, Houlton R, Burnham KE, Queree P, Sharp T. Pharmacological Evidence for 5-HT6 Receptor Modulation of 5-HT Neuron Firing in Vivo. ACS Chem Neurosci. 2015 Jul 15; 6(7):1241-7.