WAY-181187 hydrochloride  (Synonyms: SAX-187 hydrochloride)

WAY-181187 (SAX-187) hydrochloride 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^[1]. WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist^[2].

WAY-181187 (1 and 10 μM) hydrochloride increases activation of ERK1/2. WAY-181187 hydrochloride also increases Fyn kinase activity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Acute administration of WAY-181187 (3-30 mg/kg, s.c.) hydrochloride significantly increases extracellular GABA concentrations without altering the levels of glutamate or norepinephrine in the rat frontal cortex. Additionally, WAY-181187 (30 mg/kg, s.c.) hydrochloride produces modest yet significant decreases in cortical dopamine and 5-HT levels^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

417.33

C₁₅H₁₄Cl₂N₄O₂S₂

554403-08-6

NCCC1=CN(S(=O)(C2=C(Cl)N=C3SC=CN32)=O)C4=C1C=CC=C4.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Lee E Schechter, et al. Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology. 2008 May;33(6):1323-35.  [Content Brief]

  [2]. Teresa Riccioni, et al. ST1936 Stimulates cAMP, Ca2+, ERK1/2 and Fyn Kinase Through a Full Activation of Cloned Human 5-HT6 Receptors. Eur J Pharmacol. 2011 Jul 1;661(1-3):8-14.  [Content Brief]