1883548-85-3

1883548-85-3 structure

Name: WAY 181187 oxalate
Chemical Name: WAY 181187 oxalate
CAS Number: 1883548-85-3
Molecular Formula: C₁₅H₁₃ClN₄O₂S_2.C₂H₂O₄
Molecular Weight: 470.91
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2022-05-09 18:44:49
Modify Date: 2024-01-19 11:54:14
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki 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].

Name	WAY 181187 oxalate
Synonyms	1H-Indole-3-ethanamine, 1-[(6-chloroimidazo[2,1-b]thiazol-5-yl)sulfonyl]-, ethanedioate (1:1) WAY-181187 OXALATE 1-[(6-Chloroimidazo[2,1-b]thiazol-5-yl)sulfonyl]-1H-indole-3-ethanamine oxalate 2-{1-[(6-Chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonyl]-1H-indol-3-yl}ethanamine ethanedioate (1:1)

Description	WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki 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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT6 Receptor:2.2 nM (Ki) 5-HT6 Receptor:6.6 nM (EC50)
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].
References	[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. [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.