| 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].
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| Related Catalog |
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| Target |
5-HT6 Receptor:2.2 nM (Ki)
5-HT6 Receptor:6.6 nM (EC50)
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| 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.
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| 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.
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| 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.
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