A selective serotonin reuptake inhibitor
Fluvoxamineis is an antidepressant which pharmacologically functions as a selective serotonin reuptake inhibitor. Serotonin, also known as 5-HT, is amonoamine neurotransmitter with various physiological functions such as mood, appetite, and sleep[1].
In vitro: Fluvoxamine effectively inhibited 5-HT uptake by blood platelets and brain synaptosomes [1].Fluvoxamine (10 mg/kg) increased [5-HT]ex levels in all brain areas and increased [DA]ex levels in the striatum. Fluvoxamine (10 mg/kg) in combination with of quetiapine (10 mg/kg) increased [DA]ex and [5-HT]ex levels in all brain areas when compared with baseline. The combination produced a significant increase of [DA]ex levels in the prefrontal cortex and thalamus whereas neither quetiapine nor fluvoxamine in monotherapy affected [DA]ex levels [2]. Fluvoxamine induced antiallodynic effects on neuropathic pain via descending 5-HT fibers and spinal 5-HT2A or 5-HT2C receptors, and the antinociception on acute mechanical pain via 5-HT3 receptors [3].
In vivo: Single administration of fluvoxamine (10 and 30 mg/kg, i.p.) dose-dependently enhanced synaptic efficacy in the hippocampo-mPFC pathway [4]. Fluvoxamine (10 and 30 mg/kg, i.p.) treatment suppressed long-term potentiation (LTP) in the hippocampal CA1 field of anesthetized rats. NAN-190 (0.5 mg/kg, i.p), the 5-HT(1A) receptor antagonist, completely reversed the fluvoxamine (30 mg/kg, i.p.) suppression of LTP [5].
参考文献:
[1].?Claassen V,Davies JE,Hertting G,Placheta P. Fluvoxamine, a specific 5-hydroxytryptamine uptake inhibitor.Br J Pharmacol.1977 Aug;60(4):505-16.
[2].?Denys D1,Klompmakers AA,Westenberg HG. Synergistic dopamine increase in the rat prefrontal cortex with the combination of quetiapine and fluvoxamine.Psychopharmacology (Berl).2004 Nov;176(2):195-203. Epub 2004 May 11.
[3].?Honda M1,Uchida K,Tanabe M,Ono H. Fluvoxamine, a selectiveserotoninreuptake inhibitor, exerts its antiallodynic effects on neuropathic pain in mice via 5-HT2A/2C receptors.Neuropharmacology.2006 Sep;51(4):866-72. Epub 2006 Jul 17.
[4].?Ohashi S1,Matsumoto M,Otani H,Mori K,Togashi H,Ueno K,Kaku A,Yoshioka M. Changes in synaptic plasticity in the rat hippocampo-medial prefrontal cortex pathway induced by repeated treatments with fluvoxamine.Brain Res.2002 Sep 13;949(1-2):131-8.
[5].?Kojima T1,Matsumoto M,Togashi H,Tachibana K,Kemmotsu O,Yoshioka M. Fluvoxamine suppresses the long-term potentiation in the hippocampal CA1 field of anesthetized rats: an effect mediated via 5-HT1A receptors.Brain Res.2003 Jan 3;959(1):165-8.
| Animal experiment [1]: | |
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Animal models |
5-hydroxytryptamine - depleted mice |
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Dosage form |
30 mg/kg, i.p. |
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Application |
Fluvoxamine exerts its antiallodynic effects on neuropathic pain via descending 5-HT fibers and spinal 5-HT2A or 5-HT2C receptors, and the antinociception on acute mechanical pain via 5-HT3 receptors. The fluvoxamine-induced antiallodynic effect was significantly attenuated in 5-hydroxytryptamine - depleted mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1] Honda M1, Uchida K, Tanabe M, Ono H. 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. Epub 2006 Jul 17. | |
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