Bioactivity | WAY-181187 (SAX-187) hydrochloride 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]. WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[2]. |
Invitro | WAY-181187 (1 and 10 μM) hydrochloride 可增强 ERK1/2 的激活。WAY-181187 hydrochloride 还可提高 Fyn 激酶活性[2]。 |
In Vivo | WAY-181187 (3-30 mg/kg, s.c.) hydrochloride 的急性给药显着增加细胞外 GABA 浓度,而不改变大鼠额叶皮质中谷氨酸或去甲肾上腺素的水平。 此外,WAY-181187 (30 mg/kg, s.c.) hydrochloride 可适度但显着降低皮质多巴胺和 5-HT 水平[1]。 Animal Model: |
Name | WAY-181187 hydrochloride |
CAS | 554403-08-6 |
Formula | C15H14Cl2N4O2S2 |
Molar Mass | 417.33 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |