Fluvoxamine |
|
カタログ番号GC13092
|
Fluvoxamineは選択性のセロトニン(5-HT)再取り込み阻害剤(SSRI)であり、抗鬱活性を持つ。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 54739-18-3
Sample solution is provided at 25 µL, 10mM.
Fluvoxamineは選択性のセロトニン(5-HT)再取り込み阻害剤(SSRI)であり、抗鬱活性を持つ[1, 2]。Fluvoxamineはσ1受容体作動剤であり、前頭前皮質でモノアミンの細胞外レベルを増やす[3]。Fluvoxamineは、慢性ストレスのC57BL/6マウスの前頭前皮質で、5-HT3とsigma-1受容体を活性化し、よってグルタミン酸の放出を促進する[4]。
体内で、Fluvoxamine (0-50μM)で三種類のヒト神経膠芽腫細胞株(A172、U87-MGとU251-MG)を処理した結果、細胞の遊離を用量依存的に著しく阻害し、U87-MG細胞の侵入をも阻害した[5]。
体内で、Fluvoxamine (25、50、100、200mg/kg)を、胃潰瘍のラットに経口投与した結果、潰瘍の形成を著しく減らし、胃組織で抗酸化マーカー(総グルタチオンと一酸化窒素)のレベルを増やした[6]。脳虚血のラットに、Fluvoxamine (20mg/kg)を腹腔内注射した結果、運動機能を著しく改善し、梗塞体積を減らし、神経学的欠損を改善した[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.
| 細胞実験[1]: | |
細胞株 | A172、U87-MG、U251-MG細胞 |
準備方法 | A172、U87-MG、U251-MG細胞を24時間血清飢餓し、Fluvoxamine (0、25または50μM)で処理し、創傷治癒アッセイで処理した。 |
反応条件 | 0、25または50μM;24時間 |
アプリケーション | Fluvoxamineは、三種類のヒトGBM細胞株(A172、U87-MGとU251-MG)の移動を用量依存的に効果的に阻害した。 |
| 動物実験 [2]: | |
動物モデル | Wistarラット |
準備方法 | 24時間飢餓されたラットのグループに、Fluvoxamine (25、50、100と200mg/kg)、ranitidine (50mg/kg)または蒸留水を経口投与した。Indomethacin (25mg/kg)を潰瘍誘発剤として、ラットに経口投与した。潰瘍誘発の6時間後、ラットの胃を切除し、潰瘍指数を測定した。異なるグループのラットを、同じ用量のFluvoxamineとranitidine(indomethacinなし)で処理し、生物化学パラメーターのみに対するこれらの薬物の効果を調べた。胃を生物化学的に評価し、酸化と抗酸化パラメーターを測定した。 |
投与形態 | 25、50、100、200mg/kg;経口投与 |
アプリケーション | 対照のラットグループと比べて、25、50、100、200mg/kgのFluvoxamineはそれぞれ、48.5、67.5、82.1と96.1%の抗潰瘍作用を発揮した。 |
References: | |
| Cas No. | 54739-18-3 | SDF | |
| Chemical Name | 2-[(E)-[5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene]amino]oxyethanamine | ||
| Canonical SMILES | COCCCCC(=NOCCN)C1=CC=C(C=C1)C(F)(F)F | ||
| Formula | C15H21F3N2O2 | M.Wt | 318.33 |
| 溶解度 | ≥ 15.92mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1414 mL | 15.707 mL | 31.4139 mL |
| 5 mM | 628.3 μL | 3.1414 mL | 6.2828 mL |
| 10 mM | 314.1 μL | 1.5707 mL | 3.1414 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)















