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• 產(chǎn)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

• 靶點(diǎn)： 5-HT1A Receptor;5-HTReceptor

• 體外研究：
  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

• 體內(nèi)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.

• 參考文獻(xiàn)：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

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輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *