WAY 181187
WAY 181187 Basic information
- Product Name:
- WAY 181187
- Synonyms:
-
- WAY 181187
- SAX-187
- WAY181187.HCl(WAY-181,187)
- WAY-181187(SAX-187)
- WAY181187 hydrochloride
- WAY181187 HCl
- SAX-187;WAY 181187;WAY-181187(SAX-187);WAY181187 HYDROCHLORIDE
- 1H-Indole-3-ethanamine, 1-[(6-chloroimidazo[2,1-b]thiazol-5-yl)sulfonyl]-
- CAS:
- 554403-49-5
- MF:
- C15H13ClN4O2S2
- MW:
- 380.87
- Mol File:
- 554403-49-5.mol
WAY 181187 Chemical Properties
- Density
- 1.67±0.1 g/cm3(Predicted)
- solubility
- DMSO: Soluble: =10 mg/ml
- form
- Solid
- pka
- 9.30±0.10(Predicted)
- color
- White to yellow
WAY 181187 Usage And Synthesis
Uses
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].
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. |
IC 50
5-HT6 Receptor: 2.2 nM (Ki); 5-HT6 Receptor: 6.6 nM (EC50)
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. DOI:10.1038/sj.npp.1301503
[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. DOI:10.1016/j.ejphar.2011.04.028
[3] DEREK C. COLE. 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]. Journal of Medicinal Chemistry, 2007, 50 23: 5535-5538. DOI: 10.1021/jm070521y
[4] GREGORY V CARR I L Lee E Schechter. Antidepressant and anxiolytic effects of selective 5-HT6 receptor agonists in rats.[J]. Psychopharmacology, 2011, 213 2-3: 499-507. DOI: 10.1007/s00213-010-1798-7
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