Fluvoxamine is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with antidepressant activity[1, 2]. Fluvoxamine is a σ1 receptor agonist and increases the extracellular levels of monoamines in the prefrontal cortex[3]. Fluvoxamine activates 5-HT3 and sigma-1 receptors in the prefrontal cortex of C57BL/6 mice subjected to chronic stress, thereby promoting glutamate release[4].
In vitro, Fluvoxamine (0-50μM) treatment of three different human glioblastoma cell lines (A172, U87-MG, and U251-MG) significantly inhibited cell migration in a dose-dependent manner, and also inhibited U87-MG cell invasion[5].
In vivo, oral administration of Fluvoxamine (25, 50, 100, 200mg/kg) to rats with gastric ulcers significantly reduced ulceration and increased the levels of antioxidant markers (total glutathione and nitric oxide) in the gastric tissue[6]. Intraperitoneal injection of Fluvoxamine (20mg/kg) in rats with cerebral ischemia significantly improved motor function, reduced infarct volume, and ameliorated neurological deficits[7].
References:
[1] Koek W, Sandoval T L, Daws L C. Effects of the antidepressants desipramine and fluvoxamine on latency to immobility and duration of immobility in the forced swim test in adult male C57BL/6J mice[J]. Behavioural pharmacology, 2018, 29(5): 453-456.
[2] Westenberg H G M, Sandner C. Tolerability and safety of fluvoxamine and other antidepressants[J]. International Journal of Clinical Practice, 2006, 60(4): 482-491.
[3] Ago Y, Yano K, Hiramatsu N, et al. Fluvoxamine enhances prefrontal dopaminergic neurotransmission in adrenalectomized/castrated mice via both 5-HT reuptake inhibition and σ1 receptor activation[J]. Psychopharmacology, 2011, 217(3): 377-386.
[4] Fu Y, Yu S, Guo X, et al. Fluvoxamine increased glutamate release by activating both 5-HT3 and sigma-1 receptors in prelimbic cortex of chronic restraint stress C57BL/6 mice[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2012, 1823(4): 826-837.
[5] Hayashi K, Michiue H, Yamada H, et al. Fluvoxamine, an anti-depressant, inhibits human glioblastoma invasion by disrupting actin polymerization[J]. Scientific reports, 2016, 6(1): 23372.
[6] Dursun H, Bilici M, Albayrak F, et al. Antiulcer activity of fluvoxamine in rats and its effect on oxidant and antioxidant parameters in stomach tissue[J]. BMC gastroenterology, 2009, 9(1): 36.
[7] Sato S, Kawamata T, Kobayashi T, et al. Antidepressant fluvoxamine reduces cerebral infarct volume and ameliorates sensorimotor dysfunction in experimental stroke[J]. Neuroreport, 2014, 25(10): 731-736.
Fluvoxamine是一种选择性血清素（5-HT）再摄取抑制剂（SSRI），具有抗抑郁活性[1, 2]。Fluvoxamine是σ1受体的激动剂，能够增加前额叶皮层细胞外单胺的含量[3]。Fluvoxamine能够激活慢性应激C57BL/6小鼠前缘皮层中的5-HT3受体和sigma-1受体，从而促进谷氨酸的释放[4]。
在体外，Fluvoxamine（0-50μM）处理三种不同的人胶质母细胞瘤细胞系（A172U87-MG和U251-MG细胞），以剂量依赖性方式有效抑制了三种细胞的迁移，还抑制了U87-MG细胞的侵袭[5]。
在体内，Fluvoxamine（25, 50, 100, 200mg/kg）通过口服治疗胃溃疡大鼠，显著产生了抗溃疡作用，显著升高了大鼠胃组织抗氧化指标（总谷胱甘肽和一氧化氮）水平[6]。Fluvoxamine（20mg/kg）通过腹腔注射治疗脑缺血大鼠，显著改善了运动功能障碍，有效降低了脑梗塞体积并改善神经功能损伤[7]。