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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFluoxetine hydrochlorideCat. No.: HY-B0102ACAS No.: 56296-78-7Synonyms: LY-110140分式: CHClFNO分量: 345.79作靶点: Serotonin Transporter; Autophagy作通路: Neuronal Signaling; Autophagy储存式: 4C, protect from light* In solvent : -80C, 6 month

2、s; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 25 mg/mL (72.30 mM)H2O : 10 mg/mL (28.92 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8919 mL 14.4596 mL 28.9193 mL5 mM 0.5784 mL 2.8919 mL 5.7839 mL10 mM 0.2892 mL 1.4460 mL 2.89

3、19 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.23 mM); Clear solution2. 请依序添加每种溶剂: 10% DMS

4、O 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.23 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.23 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Fluoxetine hydrochloride抗抑郁药和选择性的清素重 吸收抑制剂。体外研究 Fluoxetine blocks the d

5、ownregulation of cell proliferation resulting from inescapable shock (IS) ofhippocampal cell 1. Fluoxetine increases the number of newborn cells in the dentate gyrus of thehippocampus of adult rat. Fluoxetine also increases the number of proliferating cells in the prelimbic cortex2. Fluoxetine accel

6、erates the maturation of immature neurons. Fluoxetine enhances neurogenesis-dependent long-term potentiation (LTP) in the dentate gyrus 3. Fluoxetine, but not citalopram, fluvoxamine,paroxetine and sertraline, increases norepinephrine and dopamine extracellular levels in prefrontal cortex.Fluoxetine

7、 produces robust and sustained increases in extracellular concentrations of norepinephrine anddopamine after acute systemic administration 4.体内研究 Fluoxetine treatment also reverses the deficit in escape latency observed in animals exposed to inescapableshock in adult male Sprague-Dawley rats 1. Fluo

8、xetine (5 mg/kg) alone increases cell proliferation in thedentate gyrus. Coadministration (fluoxetine 5 mg/kg + olanzapine) also significantly increases the number ofBrdU-positive cells compared with the control group 2. Fluoxetine combined with Olanzapine producesrobust, sustained increases of extr

9、acellular levels of dopamine (DA(ex) and norepinephrine (NE(ex) up to361% and 272% of the baseline, respectively, which are significantly greater than either drug alone 5.PROTOCOLAnimal Male Sprague-Dawley rats weighing 250-300 g are housed under a 12-hour light/12-hour dark cycle (lightsAdministrat

10、ion 2 on at 7:00 am, lights off at 7:00 pm) and at constant temperature (25C) and humidity and allowed freeaccess to food and water. For chronic drug treatments, rats are administered fluoxetine (5 mg/kg/day) orsaline by intraperitoneal (IP) injection once daily and olanzapine or vehicle in the drin

11、king water for 21 days(vehicle-treated control, fluoxetine, and olanzapine alone) plus the combination of fluoxetine and olanzapine.For combination treatment, olanzapine is chosen because fluoxetine is known to interfere with themetabolism of olanzapine and raise the blood levels by up to 4-6 times.

12、 Olanzapine is dissolved inhydrochloric acid (HCl), then adjusted back to pH 6 with 1 N sodium hydroxide to make the stock solution of3 mg/mL concentration. The same amount of vehicle solution is added to the water for the control animals.Fluid intake is measured three times per week, and drinking b

13、ottles are replenwashed with fresh drugsolution. There are no differences in fluid intake among the treatment groups. For subchronic treatment,drugs are administered exactly the same way but for a total period of 7 days.MCE has not independently confirmed the accuracy of these methods. They are for

14、reference only.户使本产品发表的科研献 J Neuroinflammation. 2017 Oct 30;14(1):210.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Chemosphere. 2019 Mar. Eur J Pharmacol. 2019 Jan 15;843:260-267. Behav Brain Res. 2017 Jan 15;317:62-70. Fundam Clin Pharmacol. 2018 Aug;32(4):363-377.See more customer validations

15、 on HYPERLINK / www.MedChemEREFERENCES1. Malberg JE, et al. Cell proliferation in adult hippocampus is decreased by inescapable stress: reversal by fluoxetine treatment.Neuropsychopharmacology. 2003 Sep;28(9):1562-712. Kodama M, et al. Chronic olanzapine or fluoxetine administration increases cell p

16、roliferation in hippocampus and prefrontal cortex ofadult rat. Biol Psychiatry. 2004 Oct 15;56(8):570-80.3. Wang JW, et al. Chronic fluoxetine stimulates maturation and synaptic plasticity of adult-born hippocampal granule cells. J Neurosci.2008 Feb 6;28(6):1374-84.4. Bymaster FP, et al. Fluoxetine,

17、 but not other selective serotonin uptake inhibitors, increases norepinephrine and dopamine extracellularlevels in prefrontal cortex. Psychopharmacology (Berl). 2002 Apr;160(4):353-615. Zhang W, et al. Synergistic effects of olanzapine and other antipsychotic agents in combination with fluoxetine on norepinephrine anddopamine release in rat prefrontal cortex. Neuropsychopharmacology. 2000 Sep;23(3):250-62.6. Su WJ, et al. Antidiabetic drug glyburide modulates depressive-like behavior comorbid w

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