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Fluvoxamine maleate/马来酸氟伏沙明 {[allProObj[0].p_purity_real_show]}

货号:A771257 同义名: 氟伏沙明马来酸盐 / DU-23000 maleate; Fluvoxamine (maleate)

Fluvoxamine maleate是一种选择性5-羟色胺再摄取抑制剂,可以用作抗抑郁药。。

Fluvoxamine maleate/马来酸氟伏沙明 化学结构 CAS号:61718-82-9
Fluvoxamine maleate/马来酸氟伏沙明 化学结构
CAS号:61718-82-9
Fluvoxamine maleate/马来酸氟伏沙明 3D分子结构
CAS号:61718-82-9
Fluvoxamine maleate/马来酸氟伏沙明 化学结构 CAS号:61718-82-9
Fluvoxamine maleate/马来酸氟伏沙明 3D分子结构 CAS号:61718-82-9
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Fluvoxamine maleate/马来酸氟伏沙明 生物活性

靶点
  • 5-HT

描述 Fluvoxamine maleate is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor[3]. Fluvoxamine maleate is effective in inhibiting 5-ht uptake by blood platelets and brain synaptosomes. Effects of 5-hydroxytryptophan (5-HTP) are potentiated in mice and in combination with pargyline, fluvoxamine induces 5-HT-like behavioural effects. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake[4]. Sprague-Dawley rats were treated with the antidepressant Fluvoxamine maleate (FM) prior to a unilateral 6-hydroxydopamine (6-OHDA) lesion to model motor deficits in rats[5]. Early treatment with Fluvoxamine may attenuate inflammation on injured striatal neurons by favoring anti-inflammatory cytokine expression while decreasing pro-inflammatory cytokine release in the brain[6]. The antidepressant activity and tolerability of fluvoxamine maleate (50-150 mg/day) as compared with placebo; it is also as effective as the tricyclic antidepressant imipramine (80-240 mg/day) in patients with major depressive disorder[7].

Fluvoxamine maleate/马来酸氟伏沙明 细胞实验

Cell Line
Concentration Treated Time Description References
CD4+ T cells 10 μM 48 hours To study the effect of fluvoxamine on Th1 and Th17 cell differentiation, results showed that fluvoxamine significantly repressed the number of Th1 and Th17 cells. Mol Med. 2024 Feb 5;30(1):23
N9 microglial cells 7.02 nM Fluvoxamine maleate inhibits nigericin-induced IL-1β release Front Immunol. 2024 Jul 29;15:1418422
primary astrocytes 78 nM 24 hours Fluvoxamine maleate inhibits NLRP3 inflammasome and NF-κB pathway by inducing autophagy and clears Aβ42 Front Immunol. 2024 Jul 29;15:1418422
Human peripheral blood leukocytes 20 μM 4 hours To evaluate the inhibitory effect of fluvoxamine on inflammatory response in human peripheral blood leukocytes Sci Transl Med. 2019 Feb 6;11(478):eaau5266
Human brain endothelial cells 80 nM or 400 nM 1 hour To evaluate the effect of fluvoxamine on the endosomal network in human brain endothelial cells, results showed fluvoxamine enhanced punctate labeling for EEA1 and LAMP1 Mol Psychiatry. 2024 Nov;29(11):3590-3598
PC12 cells 400 nM 20 minutes To evaluate the effect of fluvoxamine on exocytosis in PC12 cells, results showed fluvoxamine significantly accelerated the loss of intracellular fluorescence markers Mol Psychiatry. 2024 Nov;29(11):3590-3598
PC12 cells 80 nM – 2 μM 1 hour To evaluate the effect of fluvoxamine on fluid-phase uptake in PC12 cells, results showed fluvoxamine significantly increased the uptake of 4 kDa FITC-dextran at 400 nM concentration Mol Psychiatry. 2024 Nov;29(11):3590-3598

Fluvoxamine maleate/马来酸氟伏沙明 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Adult mice Intraperitoneal injection 400 nM Single injection, measured 24 hours later To evaluate the effect of fluvoxamine on blood-brain barrier permeability, results showed fluvoxamine significantly increased the accumulation of 4 kDa FITC-dextran in brain tissue Mol Psychiatry. 2024 Nov;29(11):3590-3598
Mice LPS-induced inflammation model and fecal-induced peritonitis (FIP) model Intraperitoneal injection 20 mg/kg Single or multiple doses, survival monitored To evaluate the protective effect of fluvoxamine in models of inflammation and sepsis Sci Transl Med. 2019 Feb 6;11(478):eaau5266
NOD mice Type 1 diabetes model Peritoneal injection 20 mg/kg Every other day for two weeks To study the preventive effect of fluvoxamine on type 1 diabetes, results showed that fluvoxamine significantly delayed diabetes onset and reduced incidence. Mol Med. 2024 Feb 5;30(1):23
C57BL/6 male mice DSS-induced colitis model Intraperitoneal injection 10 mg/kg/d Once daily for 3 weeks To assess the impact of antidepressants on IBD and select the most effective fluoxetine for mechanism studies. Cell Commun Signal. 2024 Mar 12;22(1):176
5XFAD transgenic mice Alzheimer disease model Oral 5 mg/kg and 10 mg/kg Once daily for two months Fluvoxamine maleate ameliorates Alzheimer disease pathology by autophagy-mediated Aβ clearance and neuroinflammation inhibition Front Immunol. 2024 Jul 29;15:1418422

Fluvoxamine maleate/马来酸氟伏沙明 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00716820 - Completed - -
NCT00716820 - Completed - -
NCT00716625 - Completed - -

Fluvoxamine maleate/马来酸氟伏沙明 参考文献

[1]Honda M, Uchida K, et al. Fluvoxamine, a selective serotonin reuptake inhibitor, exerts its antiallodynic effects on neuropathic pain in mice via 5-HT2A/2C receptors. Neuropharmacology. 2006 Sep;51(4):866-72.

[2]Denys D, Klompmakers AA, et al. Synergistic dopamine increase in the rat prefrontal cortex with the combination of quetiapine and fluvoxamine. Psychopharmacology (Berl). 2004 Nov;176(2):195-203.

[3]Ginsburg BC, Pinkston JW, Lamb RJ. The potency of fluvoxamine to reduce ethanol self-administration decreases with concurrent availability of food. Behav Pharmacol. 2012 Apr;23(2):134-42

[4]Claassen V, Davies JE, Hertting G, Placheta P. Fluvoxamine, a specific 5-hydroxytryptamine uptake inhibitor. Br J Pharmacol. 1977 Aug;60(4):505-16

[5]Dallé E, Daniels WMU, Mabandla MV. Fluvoxamine maleate effects on dopamine signaling in the prefrontal cortex of stressed Parkinsonian rats: Implications for learning and memory. Brain Res Bull. 2017 Jun;132:75-81

[6]Dallé E, Daniels WM, Mabandla MV. Fluvoxamine maleate normalizes striatal neuronal inflammatory cytokine activity in a Parkinsonian rat model associated with depression. Behav Brain Res. 2017 Jan 1;316:189-196

[7]Claghorn JL, Earl CQ, Walczak DD, Stoner KA, Wong LF, Kanter D, Houser VP. Fluvoxamine maleate in the treatment of depression: a single-center, double-blind, placebo-controlled comparison with imipramine in outpatients. J Clin Psychopharmacol. 1996 Apr;16(2):113-20

Fluvoxamine maleate/马来酸氟伏沙明 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.51mL

2.30mL

1.15mL

23.02mL

4.60mL

2.30mL

Fluvoxamine maleate/马来酸氟伏沙明 技术信息

CAS号61718-82-9
分子式C19H25F3N2O6
分子量 434.41
SMILES Code O=C(O)/C=C\C(O)=O.FC(C1=CC=C(/C(CCCCOC)=N/OCCN)C=C1)(F)F
MDL No. MFCD00269809
别名 氟伏沙明马来酸盐 ;DU-23000 maleate; Fluvoxamine (maleate); NSC 309469; MK-264; DU-23000
运输蓝冰
InChI Key LFMYNZPAVPMEGP-PIDGMYBPSA-N
Pubchem ID 9560989
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 105 mg/mL(241.71 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 20 mg/mL(46.04 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方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,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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