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Fluvoxamine maleate

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Chemical Structure| 61718-82-9 同义名 : 氟伏沙明马来酸盐 ;DU-23000 maleate;Fluvoxamine (maleate);NSC 309469;MK-264;DU-23000
CAS号 : 61718-82-9
货号 : A771257
分子式 : C19H25F3N2O6
纯度 : 99%
分子量 : 434.407
MDL号 : MFCD00269809
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
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 - -
实验方案
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
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