Fluvoxamine
(Synonyms: 氟伏沙明; DU-23000) 目录号 : GC13092
A selective serotonin reuptake inhibitor
Cas No.:54739-18-3
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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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References: [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. | |
| Cas No. | 54739-18-3 | SDF | |
| 别名 | 氟伏沙明; DU-23000 | ||
| 化学名 | 2-[(E)-[5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene]amino]oxyethanamine | ||
| Canonical SMILES | COCCCCC(=NOCCN)C1=CC=C(C=C1)C(F)(F)F | ||
| 分子式 | C15H21F3N2O2 | 分子量 | 318.33 |
| 溶解度 | ≥ 15.92mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1414 mL | 15.707 mL | 31.4139 mL |
| 5 mM | 0.6283 mL | 3.1414 mL | 6.2828 mL |
| 10 mM | 0.3141 mL | 1.5707 mL | 3.1414 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet