| 产品描述： | Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder |
| 靶点： |
5-HT1A Receptor |
| 体外研究： |
Hypidone hydrochloride inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells stably expressing hSERT with IC50 values of 1.78 nM and 1.93,respectively. Hypidone hydrochloride (0.01 nM-10 μM) concentration-dependently inhibits forskolin-stimulated cAMP formation, exerts a concentration-dependent inhibitory effect on cAMP formation with an IC50 of approximately 23.9 nM. And in antagonism studies, WAY-100635 prevents Hypidone hydrochloride-mediated inhibition of forskolin-stimulated cAMP formation. Hypidone hydrochloride shows affinities to rat 5-HT1A receptors, SERTs, NETs, and DATs, it binds to 5-HT1A receptor, serotonin transporter (SERT) with high affinity (Ki=0.19 and 0.72 nM, respectively), but its affinity to NET and DAT are low, blocking [3H]nisoxetine and [3H]win35428 binding with Ki values of 650 nM and 2652 nM respectively |
| 体内研究： |
Hypidone hydrochloride (YL0919) (oral administration; 1.25 or 5 mg/kg; 4 weeks) and fluoxetine (10 mg/kg) reverses the inhibition of locomotor activity in CUS rats. Hypidone hydrochloride (oral administration; 1.25, 2.5, and 5 mg/kg; 4 weeks) significantly reduces the immobility time in TST in mcie FST in mice. Besides, Hypidone hydrochloride displays no effect on the locomotor activity in a separate OFT. Furthermore, the antidepressant-like effect of Hypidone hydrochloride in TST and FST is completely bunted by coadministration with WAY-100635. Animal Model: Male ICR mice weighing 18–22 g Dosage: 1.25, 2.5, and 5 mg/kg Administration: Oral administration Result: Had an effect on Antidepressant-like mice in TST and FST. |
| 参考文献： |
1. Chen, H. X. et al. Antidepressant-like activity of YL-0919: a novel combined selective serotonin reuptake inhibitor and 5-HT1A receptor agonist. PloS one 8, e83271, doi:10.1371/journal.pone.0083271 (2013). 2. Qin, J. J. et al. The role of activation of the 5-HT1A receptor and adenylate cyclase in the antidepressant-like effect of YL-0919, a dual 5-HT1A agonist and selective serotonin reuptake inhibitor. Neuroscience letters 582, 104-108, 2014.09.009 (2014) |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.986 ml |
14.932 ml |
29.865 ml |
| 5 mM |
0.597 ml |
2.986 ml |
5.973 ml |
| 10 mM |
0.299 ml |
1.493 ml |
2.986 ml |
| 50 mM |
0.06 ml |
0.299 ml |
0.597 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京