盐酸氟西汀作用机制 - Medchemexpress - MCE中国

1、Product Data SheetFluoxetine hydrochlorideCat. No.: HY-B0102ACAS No.: 56296-78-7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 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 25 mg/mL (72.30 mM)

2、H2O : 10 mg/mL (28.92 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration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 2.8919 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C

3、, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。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。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Twee

4、n-80 45% salineSolubility: 2.5 mg/mL (7.23 mM); Clear solution此案可获得 2.5 mg/mL (7.23 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.23 mM); Clear

5、 solution此案可获得 2.5 mg/mL (7.23 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.23 mM); Clear solution此案可获得 2.5 mg/mL (7.23 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 10

6、0 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Fluoxetine hydrochloride (LY 110140)抗抑郁药和选择性的清素重 吸收抑制剂。体外研究 Fluoxetine hydrochloride (LY 110140) blocks the downregulation of cell proliferation resulting from inescapable shock(IS) of hippocampal cell1. Fluoxetine increases the numbe

7、r of newborn cells in the dentate gyrus of the hippocampusof adult rat. Fluoxetine also increases the number of proliferating cells in the prelimbic cortex2. Fluoxetineaccelerates the maturation of immature neurons. Fluoxetine enhances neurogenesis-dependent long-termpotentiation (LTP) in the dentat

8、e gyrus3. Fluoxetine, but not citalopram, fluvoxamine, paroxetine and sertraline,increases norepinephrine and dopamine extracellular levels in prefrontal cortex. Fluoxetine produces robust andsustained increases in extracellular concentrations of norepinephrine and dopamine after acute systemicadmin

9、istration4.体内研究 Fluoxetine hydrochloride (LY 110140) treatment also reverses the deficit in escape latency observed in animalsexposed to inescapable shock in adult male Sprague-Dawley rats1. Fluoxetine (5 mg/kg) alone increases cellproliferation in the dentate gyrus. Coadministration (fluoxetine 5 m

10、g/kg + olanzapine) also significantly increases thenumber of BrdU-positive cells compared with the control group2. Fluoxetine combined with Olanzapine producesrobust, sustained increases of extracellular levels of dopamine (DA(ex) and norepinephrine (NE(ex) up to 361%and 272% of the baseline, respec

11、tively, which are significantly greater than either drug alone5.PROTOCOLAnimal Male Sprague-Dawley rats weighing 250-300 g are housed under a 12-hour light/12-hour dark cycle (lights on atAdministration 2 7:00 am, lights off at 7:00 pm) and at constant temperature (25C) and humidity and allowed free

12、 access to food andwater. For chronic drug treatments, rats are administered fluoxetine (5 mg/kg/day) or saline by intraperitoneal (IP)injection once daily and olanzapine or vehicle in the drinking water for 21 days (vehicle-treated control, fluoxetine,and olanzapine alone) plus the combination of f

13、luoxetine and olanzapine. For combination treatment, olanzapine ischosen because fluoxetine is known to interfere with the metabolism of olanzapine and raise the blood levels by upto 4-6 times. Olanzapine is dissolved in hydrochloric acid (HCl), then adjusted back to pH 6 with 1 N sodiumhydroxide to

14、 make the stock solution of 3 mg/mL concentration. The same amount of vehicle solution is added tothe water for the control animals. Fluid intake is measured three times per week, and drinking bottles arereplenwashed with fresh drug solution. There are no differences in fluid intake among the treatm

15、ent groups. Forsubchronic 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 reference only.户使本产品发表的科研献Page 2 of 3 www.MedChemE Nat Med. 2019 Sep;25(9):1428-1441. J Neuroinflammation.

16、 2017 Oct 30;14(1):210. Chemosphere. 2019 Jun;225:378-387. Prog Neuropsychopharmacol Biol Psychiatry. 2017 Jun 15;79(Pt B):258-267. Eur J Pharmacol. 2019 Jan 15;843:260-267.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Malberg JE, et al. Cell proliferation in adult

17、 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 proliferation in hippocampus and prefrontal cortex of adult rat. BiolPsychiatry. 2004 Oc

18、t 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 Feb6;28(6):1374-84.4. Bymaster FP, et al. Fluoxetine, but not other selective serotonin uptake inhibitors, increases norepinephrine and dopamine extracellular levels inprefrontal cortex. Psychopharmacology (Berl). 2002 Apr;160(4):353-615. Z