鹽酸氟西汀作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetFluoxetine hydrochlorideCat. No.: HY-B0102ACAS No.: 56296-78-7分式: CHClFNO分量: 345.79作靶點(diǎn): Serotonin Transporter; Autophagy作通路: Neuronal Signaling; Autophagy儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C

3、, 6 months; -20C, 1 month (protect from light)。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Twee

4、n-80 45% salineSolubility: 2.5 mg/mL (7.23 mM); Clear solution此案可獲得 2.5 mg/mL (7.23 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.23 mM); Clear

5、 solution此案可獲得 2.5 mg/mL (7.23 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.23 mM); Clear solution此案可獲得 2.5 mg/mL (7.23 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 10

6、0 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Fluoxetine hydrochloride (LY 110140)抗抑郁藥和選擇性的清素重 吸收抑制劑。體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)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