WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a K i of 2.2 nM and an EC 50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
性状
Solid
IC50 & Target[1][2]
5-HT6 Receptor 2.2 nM (Ki) 5-HT6 Receptor
体外研究(In Vitro)
WAY181187 (1 and 10 μM) increases activation of ERK1/2. WAY181187 also increases Fyn kinase activity. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (262.56 mM; Need ultrasonic)配制储备液