Sertraline hydrochloride

Manufactured by Merck Group

Sourced in United States

Sertraline hydrochloride is a white crystalline powder that is a selective serotonin reuptake inhibitor (SSRI). It is used as a pharmaceutical ingredient in the production of antidepressant medications.

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Sertraline (34 citations) Hydrochlorides (2 citations)

13 protocols using sertraline hydrochloride

Sertraline Administration in Mice

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Mice received a single injection intraperitoneally (i.p.) of distilled water (10 ml/kg) or sertraline hydrochloride (Sigma, United States, dissolved in distilled water) (1 mg/ml), in a volume of 10 ml/kg of body weight. The dose was chosen on the basis of previous studies (Mouri et al., 2012 (link)).

Ma L., Xu Y., Jiang W., Li Y., Zhang X., Wang G, & Li R. (2019). Sex Differences in Antidepressant Effect of Sertraline in Transgenic Mouse Models. Frontiers in Cellular Neuroscience, 13, 24.

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Investigating Serotonin Pathway Modulation

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Serotonin hydrochloride, 5-hydroxy-3-indoleacetic acid, Nafion perfluorinated resin (5 wt.%), fluoxetine hydrochloride, and sertraline hydrochloride were purchased from Sigma-Aldrich (St. Louis, MO). Escitalopram oxalate was purchased from Tocris Bioscience (Bristol, UK). Artificial cerebrospinal fluid (aCSF) was made up of 131 mM NaCl, 2 mM KCl, 1.25 mM KH₂PO₄, 20 mM NaHCO₃, 2 mM MgSO₄, 2.5 mM CaCl₂, and 10 mM HEPES in purified (18.2 MΩ) H₂O and pH was adjusted to 7.4. A 1.0 mM stock solution of serotonin and 5-HIAA was prepared in 0.2 M HClO₄, shielded from light, and remade after 3 days. A 10 mM stock solution of each SSRI was prepared in DMSO and stored at 4°C and shielded from light. Fresh solutions of 100 nM serotonin, 1 μm 5-HIAA and 10 μm SSRI were prepared the day of each experiment.

Stucky C, & Johnson M.A. (2022). Improved Serotonin Measurement with Fast-Scan Cyclic Voltammetry: Mitigating Fouling by SSRIs. Journal of the Electrochemical Society, 169(4), 045501.

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Antidepressant Delivery Routes Evaluation

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7–10 days postsurgery (or in age matched non-surgical controls) oral drug treatment delivery began. All oral delivery of antidepressants was via the drinking water. Animals randomized to the fluoxetine group received fluoxetine hydrochloride (Sigma Millipore) at a calculated individual dose of 18 mg/kg for 14 days^{19 (link)}. Those in the oral sertraline group received sertraline hydrochloride (Sigma Millipore) at a dose of 6 mg/kg for 14 days, while those in the sertraline injected group received a single i.p. injection at a dose of 20 mg/kg 30 m prior to behavioural testing^{19 (link)}. Mice in the bupropion group received bupropion hydrochloride (Sigma Millipore) at a dose of 6 mg/kg for 14 days^{20 (link)}.

McVey Neufeld K.A., Bienenstock J., Bharwani A., Champagne-Jorgensen K., Mao Y., West C., Liu Y., Surette M.G., Kunze W, & Forsythe P. (2019). Oral selective serotonin reuptake inhibitors activate vagus nerve dependent gut-brain signalling. Scientific Reports, 9, 14290.

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Sertraline-Cyclodextrin Inclusion Complex

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Sertraline hydrochloride (1S,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride, SRT, 342.69 g∙mol⁻¹, 0.98 mass fraction purity) and randomly methylated β-cyclodextrin with Average Degree of Substitution DS ~12.5 (RMβCD) (~1310 g∙mol⁻¹, 0.98 mass fraction purity) were purchased from Sigma-Aldrich (USA) or CycloLab (Hungary). The substances were used without any additional purifications. The solid substances were dried at 298 K for 72 h under reduced pressure. The water content in the cyclodextrin under investigation was determined as described previously [72 (link)]. Water used in the isothermal titration calorimetry and the circular dichroism spectroscopy measurements was distilled three times and degassed prior to experiments.

Belica-Pacha S., Daśko M., Buko V., Zavodnik I., Miłowska K, & Bryszewska M. (2021). Thermodynamic Studies of Interactions between Sertraline Hydrochloride and Randomly Methylated β-Cyclodextrin Molecules Supported by Circular Dichroism Spectroscopy and Molecular Docking Results. International Journal of Molecular Sciences, 22(22), 12357.

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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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Comparative Evaluation of PL-Inducing Agents

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The PL-inducing agents and other compounds tested in the assays, including amikacin, amiodarone hydrochloride, sertraline hydrochloride, and acetaminophen, were purchased from Sigma-Aldrich (St. Louis, MO, USA). Information about each of these drugs can be found in prior reports [7 (link),35 (link)]. amikacin, amiodarone, and sertraline are weak, moderate and strong PL-inducing drugs, respectively. acetaminophen was used as a negative control drug for the induction of PL. All other compounds and reagents used in the analyses were obtained at an analytical grade from common commercial sources.

Lee J.Y., Han H.J., Lee S.J., Cho E.H., Lee H.B., Seok J.H., Lim H.S, & Son W.C. (2020). Use of 3D Human Liver Organoids to Predict Drug-Induced Phospholipidosis. International Journal of Molecular Sciences, 21(8), 2982.

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Antidepressant Treatments in Mice

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Desipramine hydrochloride, sertraline hydrochloride, and aripiprazole were purchased from Sigma-Aldrich, Tokyo Chemical Industry Co, Ltd, and Wako Pure Chemical Industries, Ltd, respectively. Desipramine and sertraline were dissolved in distilled water. aripiprazole was dissolved in 100% acetic acid and diluted with distilled water.
From 1 day after the last social defeat stress exposure, i.p. administration of 10 and 20 mg/kg desipramine, 5 and 10 mg/kg sertraline, or 0.003 and 0.01 mg/kg aripiprazole was commenced; this treatment was performed once a day for 15 days. The administration volume was 10 mL/kg per mouse.

Hasegawa S., Miyake Y., Yoshimi A., Mouri A., Hida H., Yamada K., Ozaki N., Nabeshima T, & Noda Y. (2018). Dysfunction of Serotonergic and Dopaminergic Neuronal Systems in the Antidepressant-Resistant Impairment of Social Behaviors Induced by Social Defeat Stress Exposure as Juveniles. International Journal of Neuropsychopharmacology, 21(9), 837-846.

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Cytotoxicity Assay Protocol

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The following chemical reagents were used in this study: BI2536 and cisplatin (Selleckchem, Houston, TX, USA). DHA, sertraline hydrochloride, and rapamycin (Sigma-Aldrich, USA), and thioridazine (Tocris, UK)

Lee H.J., Song K.H., Oh S.J., Kim S., Cho E., Kim J., Park Y.G., Lee K.M., Yee C., Song S.H., Chang S., Choi J., Jung S.T, & Kim T.W. (2022). Targeting TCTP sensitizes tumor to T cell-mediated therapy by reversing immune-refractory phenotypes. Nature Communications, 13, 2127.

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Evaluating Antidepressant Effects on Cell Adhesion

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For drug exposure experiments, fluoxetine hydrochloride and sertraline hydrochloride (Sigma-Aldrich) were solubilized in dimethyl sulfoxide (DMSO) and diluted in cell culture media to the stated concentration/dosage. DMSO was controlled in all experiments such that higher drug concentrations did not necessarily indicate higher DMSO dosages, with all media containing <1% DMSO. For all exposure experiments, media was replenished daily to simulate clinical administration of drugs.
To determine concentrations of intercellular adhesion molecule-1 (ICAM), vascular cell adhesion molecule-1 (VCAM), and transforming growth factor beta-1 (TGFβ), ELISAs were performed. DuoSet kits (R&D Systems) for each target were purchased and used per manufacturer’s protocols. At each time point, cell culture supernatant was collected, spun at 10,000g for 10 min at 4°C, then frozen at −80°C. Samples were thawed at room temperature prior to running each assay. Absorbance was measured via plate reader.

Arumugasaamy N., Gudelsky A., Hurley-Novatny A., Kim P.C, & Fisher J.P. (2019). Placental Barrier Phenotypic Response to Fluoxetine and Sertraline: A Comparative Study. Advanced healthcare materials, 8(18), e1900476.

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Sertraline Susceptibility Bioscreen Assay

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We performed Bioscreen growth assays to assess the susceptibility of the different strains to sertraline (sertraline hydrochloride; Sigma-Aldrich). Growth assays covered a wide range of concentrations (for each compound/strain, we initially performed an exploratory experiment to define an optimal range including nine concentrations) for each compound of interest using three biological replicates (each one with three replicates for a total of nine replicates) per strain/concentration. Growth was defined as the instances in which two or more replicates increased their OD₆₀₀ more than twice the maximum OD₆₀₀ increment of the control wells (inoculated with sterile LB medium) after 16 h of incubation.

Arrieta-Ortiz M.L., Pan M., Kaur A., Pepper-Tunick E., Srinivas V., Dash A., Immanuel S.R., Brooks A.N., Shepherd T.R, & Baliga N.S. (2022). Disrupting the ArcA Regulatory Network Amplifies the Fitness Cost of Tetracycline Resistance in Escherichia coli. mSystems, 8(1), e00904-22.

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