氟伏沙明馬來酸鹽作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetFluvoxamine maleateCat. No.: HY-B0103ACAS No.: 61718-82-9分式: CHFNO分量: 434.41作靶點(diǎn): Serotonin Transporter作通路: Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (230.20 mM)H2O : 20 mg/mL (46.04 mM; Need ultrasonic)* means

2、 soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.3020 mL 11.5099 mL 23.0197 mL5 mM 0.4604 mL 2.3020 mL 4.6039 mL10 mM 0.2302 mL 1.1510 mL 2.3020 mL請根據(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, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C

3、儲(chǔ)存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.75 mM); Clear solution此案可獲得 2.

4、5 mg/mL (5.75 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. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.75 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.75 mM，飽和度未知) 的澄清溶液

5、。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.75 mM); Clear solution此案可獲得 2.5 mg/mL (5.75 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 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。4. 請依序添加每種溶劑： PBS5.Solubil

6、ity: 20 mg/mL (46.04 mM); Clear solution; Need ultrasonic請依序添加每種溶劑： phosphate buffer salineSolubility: 20 mg/mL (46.04 mM); Clear solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 Fluvoxamine maleate (DU-23000 maleate)5-羥胺再吸收抑制劑，有抗抑郁活性。IC & Target SSRIs1.體內(nèi)研究 Fluvoxamine maleate (DU-23000 maleate) is

7、effective in inhibiting 5-ht uptake by blood platelets and brainsynaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazoleconvulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects ofdesmethylimipramine and

8、imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-likecompounds are given following a dose of fluvoxamine1. Fluvoxamine (DU-23000) appears to improve combat-related PTSD symptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits

9、theconclusions of our study. Controlled studies of fluvoxamine in the treatment of PTSD are warranted2. Fluvoxamine(DU-23000) was less potent at decreasing ethanol self-administration when food was available concurrently versuswhen ethanol was available in isolation ED50: 4.0 (2.7-5.9) and 5.1 (4.3-

10、6.0). Effects on food were similar under eachcondition in which food was available. The results demonstrate that the potency of fluvoxamine in reducing ethanol-maintained behavior depends on whether ethanol is available in isolation or in the context of concurrently scheduledfood reinforcement3.戶使本產(chǎn)

11、品發(fā)表的科研獻(xiàn) Sci Transl Med. 2019 Feb 6;11(478). pii: eaau5266. PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Ginsburg, B.C., J.W. Pinkston, and R.J. Lamb, The potency of fluvoxamine to reduce ethanol self-administration de

12、creases with concurrent availability offood. Behav Pharmacol, 2012. 23(2): p. 134-42.2. Claassen, V., et al., Fluvoxamine, a specific 5-hydroxytryptamine uptake inhibitor. Br J Pharmacol, 1977. 60(4): p. 505-16.3. Escalona, R., et al., Fluvoxamine treatment in veterans with combat-related post-traumatic stress disorder. Depress Anxiety, 2002. 15(1): p. 29-33.Page 2 of 3 www.MedChemEMcePdfHeightCaution: Product has not b