WAY-181187 (SAX-187) oxalate 是一种有效的选择性全 5-HT6 受体激动剂,Ki 为 2.2 nM,EC50 为 6.6 nM。
Cas No. | 1883548-85-3 |
别名 | SAX-187 oxalate |
Canonical SMILES | NCCC2=CN(S(C3=C(Cl)N=C4N3C=CS4)(=O)=O)C1=CC=CC=C12.O=C(O)C(O)=O |
分子式 | C15H13ClN4O2S2.C2H2O4 |
分子量 | 470.91 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | High affinity and selective 5-HT6 agonist (Ki = 2.2 nM). Displays 60-fold selectivity over other 5-HT and monoamine receptors. Increases firing rate of 5-HT neurons. Modifies sleep and wakefulness profiles following direct injections into the dorsal raphe nucleus, in vivo. Orally bioavailable. Brouard et al (2015) Pharmacological evidence for 5-HT6 receptor modulation of 5-HT neuron firing in Vivo. ACS Chem.Neurosci. 6 1241 PMID:25837696 |Cole et al (2007) Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT6 receptor agonist. J.Med.Chem. 50 5535 PMID:17948978 |