DOV-216-303-Free-Base - Serotonin Transporter 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDOV-216,303 Free BaseCat. No.: HY-18332CCAS No.: 66504-40-3分式: CHClN分量: 228.12作靶點(diǎn): Serotonin Transporter; Dopamine Transporter作通路: Neuronal Signaling儲(chǔ)存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實(shí)驗(yàn) DMSO : 125 mg/mL (547.96 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (9.12 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (9.12 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 DOV-216,303 (Free Base)有效的

3、 5-羥胺、去甲腎上腺素、多巴胺再攝取的三重 抑制劑，其對 hSERT、hNET 和 hDAT 的 IC50 值分別為 14 nM，20 nM和78 nM 1。在嗅球切除模型中，可增加前額質(zhì)中單胺的釋放及具有抗抑郁的作 2。IC50 & Target IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine) 1.體內(nèi)研究 Acute treatment of DOV-216,303 (20 mg/kg, i.p.) significantly increases dopamine, norepinephrine ands

4、erotonin levels in both OBX and Sham animals 2.Chronic treatment with DOV 216,303 (20 mg/kg, i.p., for 17 days) increases extracellular concentrations ofdopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals andsignificantly increases extracellular baseli

5、ne serotonin concentrations 2.Animal Model: Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Shamsurgery 2.Dosage: 20 mg/kg.Administration: I.P. daily for 17days.Result: Increased extracellular concentrations of dopamine, norepinephrine and serotonin in themedial prefrontal

6、cortex of both OBX and Sham animals and significantly increasedextracellular baseline serotonin concentrations.Animal Model: Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Shamsurgery 2.Dosage: 20 mg/kg.Administration: I.P. once.Result: Significant increases in dopamine, n

7、orepinephrine and serotonin levels were measuredin both OBX and Sham animals.REFERENCES1. Shao L, et al. Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopaminereuptake inhibitor. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1438-41.2. Prins J, et al. The putative antidepressant DOV 216,303, a triple reuptake inhibitor, increases monoamine release in the prefrontal cortexof olfactory bulbectomized rats. Eur J Pharmacol. 2010 May 10;633(1-3):55-61.McePdfHeightCaution: Product has not been fully validated for medical applications.For