Fluvoxamine maleate

Manufactured by Merck Group

Sourced in United States

Fluvoxamine maleate is a pharmaceutical compound used as an active ingredient in various medications. It is a selective serotonin reuptake inhibitor (SSRI) that can be used to treat certain medical conditions. This product is intended for use in a laboratory setting for research and development purposes.

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Lab products found in correlation

Venlafaxine hydrochloride, by Merck Group (3 mentions) Fluoxetine hydrochloride, by Merck Group (3 mentions) Citalopram hydrobromide, by Merck Group (3 mentions) Formic acid, by Thermo Fisher Scientific (3 mentions) Chlorzoxazone, by Merck Group (2 mentions) Tacrine hydrochloride, by Cayman Chemical (2 mentions) Diazepam, by Merck Group (2 mentions) Fluoxetine hcl, by Merck Group (2 mentions) Sertraline hydrochloride, by Merck Group (2 mentions) Paroxetine hydrochloride, by Merck Group (2 mentions) Pierce bca protein assay kit, by Thermo Fisher Scientific (2 mentions) Phenacetin, by Merck Group (1 mentions) Dimethyl sulfoxide (dmso), by Loba Chemie (1 mentions) 1 hydroxytacrine, by Cayman Chemical (1 mentions) Methanol and acetonitrile hplc grade, by Thermo Fisher Scientific (1 mentions) Peg 400, by Loba Chemie (1 mentions) Direct q3, by Merck Group (1 mentions) Nicotinamide adenine dinucleotide phosphate nadph, by Merck Group (1 mentions) Tween 20, by Merck Group (1 mentions) α naphthoflavone, by Merck Group (1 mentions)

12 protocols using fluvoxamine maleate

In Vitro Metabolism of Pinocembrin

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Pinocembrin
(≥95%), tacrine hydrochloride (≥98%), hydroxytacrine
maleate, i.e., 1-hydroxytacrine (≥98%), and
paracetamol (≥98%) were obtained from Cayman Chemical. Fluvoxamine
maleate (≥97%), phenacetin (≥98%), diazepam (∼98%),
chlorzoxazone (≥98%), nicotinamide adenine dinucleotide phosphate
(NADPH) (≥98%), and Tween 20 were procured from Sigma-Aldrich.
Caffeine was obtained from the Indian Pharmacopoeia Commission. RLM
(lot no. RT059-D) and HLM (pool of 50 donors; lot no. PL050D-A) were
procured from Gibco. MS-grade acetonitrile and formic acid as well
as HPLC-grade methanol and acetonitrile were obtained from Thermo
Fisher Scientific. Magnesium chloride and monobasic potassium phosphate
were purchased from Rankem. PEG-400 and dimethylsulfoxide (DMSO) were
procured from Loba Chemie. Ultrapure water was obtained from a water
purification system (Direct-Q 3, Merck-Millipore). Characterization
data of the test candidate (pinocembrin) are presented in Figures S1–S4.

Bhatt S., Dhiman S., Kumar V., Gour A., Manhas D., Sharma K., Ojha P.K, & Nandi U. (2022). Assessment of the CYP1A2 Inhibition-Mediated Drug Interaction Potential for Pinocembrin Using In Silico, In Vitro, and In Vivo Approaches. ACS Omega, 7(23), 20321-20331.

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Measuring Enzyme Inducibility and Activity

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Example 7

Measuring Inducibility and Activity of CYP1A1/B1, CYP1A2, and CYP2B6 Enzymes

Metabolic capability of both culture systems is further confirmed by examining inducibility and activity of CYP1A1/B1, CYP1A2, and CYP2B6 enzymes using P450-Glo Assays (Promega) according to the manufacturer's instruction. CYP activities are induced 48 hours prior measurement with a combination of 10 nM Tetrachlorodibenzodioxin (TCDD) and 25 μM rifampicin (Sigma-Aldrich, Buchs, Switzerland). 20 μM α-naphthoflavone and 10 μM fluvoxamine maleate (Sigma) are used to inhibit CYP1A1/B1 and CYP2B6 activities, respectively. Once the measurements are completed, tissues are washed twice with PBS and returned to the incubator.

US11041145B2. Cell culture (2021-06-22). PHILIP MORRIS PRODUCTS S.A. [CH]. Inventors: David Bovard [CH], Karsta Luettich [CH].

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Desipramine and Fluvoxamine Administration

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Desipramine (desmethylimipramine) hydrochloride and fluvoxamine maleate (Sigma-Aldrich, St. Louis, MO) were dissolved in physiological saline and injected i.p. at doses expressed as base weight per kg body weight. The injection volume was 10 ml/kg.

Koek W., Sandoval T.L, & Daws L.C. (2018). 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. Behavioural pharmacology, 29(5), 453-456.

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Hepatocyte Isolation and Characterization

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Tacrine hydrochloride and MK571 were obtained from Cayman Chemical Company (Ann Arbor, MI). Collagenase (type I, class I), rat tail collagen (type I), Dulbecco’s modified Eagle’s medium (DMEM), and insulin were purchased from Invitrogen (Carlsbad, CA). Fluvoxamine maleate, verapamil hydrochloride, 5 - (and – 6) – carboxy - 2’, 7 ’-dichlorofluorescein diacetate (CDFDA), dexamethasone, tetraethylammonium chloride (TEA), bovine serum albumin (BSA), soybean trypsin inhibitor, and fetal bovine serum (FBS) were purchased from Sigma-Aldrich (St. Louis, MO). ITS culture supplement (10μg/ml insulin, 10μg/ml transferrin, 10ng/ml selenous acid) was obtained from BD Biosciences (San Jose, CA). Valspodar was obtained from XenoTech (Lenexa, KS). Total protein measurement’s reagents with the bicinchoninic acid (BCA) method were from Pierce (Rockford, IL). All other chemicals and reagents were of analytical grade and were readily available from commercial sources.

Mohamed L.A, & Kaddoumi A. (2014). Tacrine Sinusoidal Uptake and Biliary Excretion in Sandwich-Cultured Primary Rat Hepatocytes. Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques, 17(3), 427-438.

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Ropinirole Metabolism in Human and Canine Hepatocytes

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Ropinirole HCl, β‐nicotinamide adenine dinucleotide 2′‐phosphate (NADPH) and fluvoxamine maleate were purchased from Sigma‐Aldrich (St. Louis, MO, USA). Despropyl ropinirole HCl and 7‐hydroxy ropinirole HBr were purchased as reference standards from TLC Pharmaceutical Standards LTD (Aurora, ON, Canada). All solvents used were of analytical grade. The stock solutions of ropinirole and fluvoxamine were prepared in purified (MilliQ) water and the metabolite standards in methanol.
Human and dog hepatocytes, as well as Krebs–Henseleit buffer (KHB), were purchased from BioIVT (Westbury, NY, USA). The dog hepatocytes were a pool of four male beagles, whereas human hepatocytes were a mixed gender pool of 50 donors. Canine recombinant CYP (rCYP) Bactosomes (co‐expressed with dog CYP reductase in Escherichia coli) were obtained from Cypex LTD (Dundee, Scotland). Ropinirole was tested in all available canine CYP isoforms (CYP1A1, CYP1A2, CYP1B1, CYP2C11, CYP2C21, CYP2C41, CYP2D15, CYP3A12 and CYP3A26).

Tervahauta T., Uutela P, & Koskinen M. (2023). Metabolism of ropinirole is mediated by several canine CYP enzymes. Veterinary Medicine and Science, 9(4), 1584-1591.

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Serotonin Reuptake Inhibitor Protocols

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Escitalopram oxalate was a generous gift from H. Lundbeck USA (Paramus, NJ). [³H]-citalopram was obtained from Amersham (Piscataway, NJ). Fluoxetine HCl and fluvoxamine maleate were obtained from Sigma-Aldrich (St. Louis, MO). All drugs administered to animals were dissolved in sterile saline.

Murray K.E., Ressler K.J, & Owens M.J. (2015). In Vivo Investigation of Escitalopram’s Allosteric Site on the Serotonin Transporter. Pharmacology, biochemistry, and behavior, 141, 50-57.

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Neurotransmitter Binding Assay

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³H-serotonin (80 Ci/mmol), ³H-norepinephrine (20 Ci/mmol), and ³H-dopamine (60 Ci/mmol) were purchased from M.G.P. (Zlín, Czech Republic). Forskolin was obtained from Scintila, s.r.o. (Jihlava, CZ). Paroxetine hydrochloride, citalopram hydrobromide, sertraline hydrochloride, fluoxetine hydrochloride, fluvoxamine maleate, venlafaxine hydrochloride, phenelzine sulfate salt, entacapone, GBR 12935 dihydrochloride, nisoxetine hydrochloride, hydrocortisone, and decynium-22 were purchased from Sigma-Aldrich (St. Louis, USA). Pierce™ BCA Protein Assay Kit was purchased from Thermo Fisher Scientific (Waltham, United States). All other chemicals were of analytical grade.

Vachalova V., Karahoda R., Ottaviani M., Anandam K.Y., Abad C., Albrecht C, & Staud F. (2022). Functional reorganization of monoamine transport systems during villous trophoblast differentiation: evidence of distinct differences between primary human trophoblasts and BeWo cells. Reproductive Biology and Endocrinology : RB&E, 20, 112.

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Radioligand Binding Assays for Monoamine Transporters

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All SSRIs (alaproclate-HCl, citalopram-HBr, fluvoxamine-maleate, fluoxetine-HCl, norfluoxetine-HCl, paroxetine-HCl, sertraline-HCl) and other monoamine transporter inhibitors (imipramine-HCl, desipramine-HCl, clomipramine-HCl, maprotiline-HCl) were obtained from Sigma-Aldrich (St. Louis, USA). [¹²⁵I]MIBG (specific activity ≈ 0.65 TBq/mmol) was purchased from Chelatec (Saint-Herblain, France). [³H]Serotonin (5-hydroxytryptamine creatinine sulfate, specific activity ≈ 3.84 TBq/mmol) was purchased from PerkinElmer.

Blom T., Meinsma R., Rutgers M., Buitenhuis C., Dekken-Van den Burg M., van Kuilenburg A.B, & Tytgat G.A. (2020). Selective serotonin reuptake inhibitors (SSRIs) prevent meta-iodobenzylguanidine (MIBG) uptake in platelets without affecting neuroblastoma tumor uptake. EJNMMI Research, 10, 78.

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Fluvoxamine Dose-Dependent Effects on Compulsive-Like Behaviors

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Fluvoxamine maleate (Sigma Aldrich) was dissolved in physiological saline (pH=7.4) to yield final doses of 10 mg/kg, 20 mg/kg and 40 mg/kg (pH 7–7.4). Saline served as a vehicle (0 mg/kg) control. All male compulsive-like mice were divided into four treatment groups (starting at 12 animals per group) comprising vehicle (sterile saline with pH adjusted to 7.4), 10 mg/kg, 20 mg/kg and 40 mg/kg fluvoxamine. Animals in each group received subcutaneous injections of fluvoxamine/vehicle daily for 17 days.

Mitra S, & Bult-Ito A. (2018). Attenuation of compulsive-like behavior by fluvoxamine in a non-induced mouse model of obsessive-compulsive disorder. Behavioural pharmacology, 29(4), 299-305.

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Cytochrome P450 Inhibition Assay Protocol

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Flucloxacillin (CAS: 1847‐24‐1) was a kind gift of Dr Bayliss from the University of Liverpool. β‐Nicotinamide adenine dinucleotide phosphate disodium salt (NADP; CAS: 24292‐60‐2), glucose‐6‐phosphate (G‐6‐P; CAS: 54010‐71‐8), G‐6‐P dehydrogenase from baker's yeast (

Saccharomyces cerevisiae

; CAS: 9001‐40‐5), (+)‐N‐3‐benzyl‐nirvanol (CAS: 790676‐40‐3), bufuralol (CAS: 60398‐91‐6), chlorzoxazone (CAS: 95‐25‐0), diethyldithiocarbamate (CAS: 20624‐25‐3), fluvoxamine maleate (CAS: 22916‐47‐8), ketoconazole (CAS: 65277‐42‐1), (S)‐mephenytoin (CAS: 70989‐04‐7), miconazole (CAS: 22916‐47‐8), α‐naphtoflavone (CAS: 604‐59‐1), quercetin (CAS: 6151‐25‐3), quinidine (CAS: 56‐54‐2), sulfaphenazole (CAS: 526‐08‐9), testosterone (CAS: 58‐22‐0), ticlopidine (CAS: 53885‐35‐1) and troleandomycin (CAS: 2751‐09‐9) were purchased from Sigma‐Aldrich (St. Louis, MO, USA). Midazolam (CAS: 59467‐96‐8) was from Duchefa Farma (Haarlem, the Netherlands). All other chemicals were of analytical grade purity and obtained from standard suppliers.

Dekker S.J., Dohmen F., Vermeulen N.P, & Commandeur J.N. (2018). Characterization of kinetics of human cytochrome P450s involved in bioactivation of flucloxacillin: inhibition of CYP3A‐catalysed hydroxylation by sulfaphenazole. British Journal of Pharmacology, 176(3), 466-477.

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