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WAY-181187 oxalate

Names

[ CAS No. ]:
1883548-85-3

[ Name ]:
WAY-181187 oxalate

[Synonym ]:
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)

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H13ClN4O2S2.C2H2O4

[ Molecular Weight ]:
470.91

[ Exact Mass ]:
470.012146

Related Compounds