554403-49-5
554403-49-5 structure
- Name: WAY-181187
- Chemical Name: 2-[1-(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonylindol-3-yl]ethanamine
- CAS Number: 554403-49-5
- Molecular Formula: C15H13ClN4O2S2
- Molecular Weight: 380.87200
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2018-12-25 10:39:10
- Modify Date: 2025-08-23 17:07:37
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WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM[1]. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[2].
| Name | 2-[1-(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonylindol-3-yl]ethanamine |
|---|---|
| Synonyms |
way-181187
unii-wxe3h7w295 |
| Description | WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM[1]. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[2]. |
|---|---|
| Related Catalog | |
| Target |
5-HT6 Receptor:2.2 nM (Ki) 5-HT6 Receptor:6.6 nM (EC50) |
| In Vitro | WAY181187 (1 and 10 μM) increases activation of ERK1/2. WAY181187 also increases Fyn kinase activity[2]. Western Blot Analysis[2] Cell Line: HEK/HA-5-HT6 receptor cells Concentration: 1 and 10 μM Incubation Time: Pretreatment 5 minutes Result: Increased activation of ERK1/2 both at 1 and 10 μM concentrations. |
| In Vivo | Acute administration of WAY-181187 (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 (30 mg/kg, s.c.) produces modest yet significant decreases in cortical dopamine and 5-HT levels[1]. Animal Model: Adult male Sprague-Dawley rats weighing 280–350 g[1] Dosage: 3, 10, or 30 mg/kg Administration: Acute dministered by s.c. Result: Significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine. |
| References |
| Molecular Formula | C15H13ClN4O2S2 |
|---|---|
| Molecular Weight | 380.87200 |
| Exact Mass | 380.01700 |
| PSA | 119.01000 |
| LogP | 4.52320 |