Desloratadine

Manufactured by Merck Group

Sourced in United States

Desloratadine is a synthetic organic compound used in the production of pharmaceutical drugs. It is a histamine H1 receptor antagonist, primarily utilized as an active ingredient in antihistamine medications. The core function of Desloratadine is to block the effects of histamine, a chemical involved in the body's immune response, thereby reducing symptoms associated with allergic reactions.

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Lab products found in correlation

7 protocols using desloratadine

Compound Solubilization and Characterization

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Compounds were obtained from ThermoFisher Scientific (amitriptyline hydrochloride, carbamazepine) and Sigma-Aldrich (chlorpromazine hydrochloride, chlorpromazine sulfoxide, clemastine fumarate salt, des loratadine, haloperidol, imipramine hydrochloride, loratadine, remdesivir, terfenadine, camostat mesylate and E64D). All compounds were solubilized in dimethyl sulfoxide (DMSO). The final concentration of DMSO was 0.01% for all experiments.

Morin-Dewaele M., Bartier S., Berry F., Brillet R., López-Molina D.S., Nguyễn C.T., Maille P., Sereno K., Nevers Q., Softic L., Vaugeois J.M., Louis B., Bequignon E., Bruscella P., Coste A., Pawlotsky J.M., Jamain S, & Ahmed-Belkacem A. (2022). Desloratadine, an FDA-approved cationic amphiphilic drug, inhibits SARS-CoV-2 infection in cell culture and primary human nasal epithelial cells by blocking viral entry. Scientific Reports, 12, 21053.

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Mast Cell Activation Assay

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Anti-DNP IgE antibody (monoclonal anti-dinitrophenyl antibody produced in mouse, IgE isotype, clone SPE-7), Evans blue, disodium cromoglycate, Desloratadine and formamide were purchased from Sigma Aldrich (Sigma-Aldrich, Co., St. Louis, MO). DNP-BSA (DNP-Albumin Conjugate, Bovine) was from Calbiochem (EMD Chemicals, Inc., San Diego, CA). Formoterol fumarate and Fostamatinib were synthesized at the Department of Chemical Research, Boehringer Ingelheim Pharma GmbH and Co. KG (Biberach, Germany). Hydroxyethylcellulose was from Merck (Merck Schuchardt OHG, Hohenbrunn, Germany). Tween20 was purchased from Acros Organics (New Jersey, USA). Narcoren was from Merial GmbH (Halbergmoos, Germany). Isoflurane (Forene) was from Abbott (Wiesbaden, Germany). Ketamine hydrochloride (Ketavet) was purchased from Pfizer Pharmacia GmbH (Berlin, Germany). Pancuronium bromide (Pancuronium Inresa) was from Inresa Arzneimittel GmbH (Freiburg, Germany).

Wex E., Thaler E., Blum S, & Lamb D. (2014). A Novel Model of IgE-Mediated Passive Pulmonary Anaphylaxis in Rats. PLoS ONE, 9(12), e116166.

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Procurement of Pharmaceutical Compounds

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Amitriptyline, cyclobenzaprine hydrochloride, cyproheptadine, des loratadine, ketotifen, loratadine, nortriptyline, and pizotifen were purchased from Sigma Chemical (St. Louis, MO, USA). Azatadine was obtained from The United States Pharmacopeial Convention (USP; Rockville, MD, USA) and deptropine citrate from the European Directorate for the Quality of Medicines (EDQM; Strasbourg, France). Amineptine and rupatadine fumarate were purchased from Toronto Research Chemicals (North York, ON, Canada), and sorafenib and erlotinib were purchased from Cayman Chemical (Ann Arbor, MI, USA).

Liang Y.C., Chang C.C., Sheu M.T., Lin S.Y., Chung C.C., Teng C.T, & Suk F.M. (2020). The Antihistamine Deptropine Induces Hepatoma Cell Death through Blocking Autophagosome-Lysosome Fusion. Cancers, 12(6), 1610.

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Quantification of Amine Oxidase Activity

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Aminoantipyrine (AAP), ammonia assay kit, bovine serum albumin (BSA), broad range SDS-PAGE molecular weight standards, concanavalin-A coupled with fluorophore fluorescein isothiocyanate (Con-A-FITC), desloratadine, 3,5-dichloro-2-hydroxybenzoic acid (DCHBS), histamine, hydrogen peroxide (H₂O₂), homovanillic acid (HVA), paraformaldehyde, horseradish peroxidase (HRP) type II, HRP type X, pig kidney diamine oxidase (pkDAO), protease inhibitor cocktail, putrescine, pyridoxal 5′-phosphate (PLP), semicarbazide and N-nitro-L-arginine methyl ester (L-NAME) were purchased from Sigma-Aldrich (Oakville, Ontario, Canada). Bradford reagent, acrylamide/bis-acrylamide solution (29:1) and Precision plus Protein Kaleidoscope Standards were from Bio-Rad Laboratory (Mississauga, Ontario, Canada). All current chemicals were Reagent Grade and were used without further purification.

Neree A.T., Soret R., Marcocci L., Pietrangeli P., Pilon N, & Mateescu M.A. (2020). Vegetal diamine oxidase alleviates histamine-induced contraction of colonic muscles. Scientific Reports, 10, 21563.

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Antihistamine Receptor Binding Assay

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Bilastine was supplied by Faes Farma (Leioa, Spain). Fexofenadine hydrochloride and olopatadine hydrochloride were from Cayman Chemical (Ann Arbor, MI, USA). Oxatomide was from Toronto Research Chemicals (North York, ON Canada). Levocetiridine dihydrochloride was from Combi-Blocks (San Diego, CA, USA). Bepotastine beslilate was from ChemScence (Monmouth Junction, NJ, USA). Rupatadine fumarate was from MedChemexpress (Monmouth Junction, NJ, USA). Desloratadine was from Sigma-Aldrich (St, Louis, MO, USA). myo-[³H]-inositol (37kBq/well) and Insta-Gel Plus scintillation cocktail were from PerkinElmer (Waltham, MA, USA). AG 1-X8 (200–400 mesh formate form) was from Bio-Rad (Richmond, CA, USA). The predeveloped TaqMan Assay Reagent of human glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was from Applied Biosystems (Foster City, CA, USA). Minimal essential medium-α (MEM-α) was from Invitrogen (Carlsbad, CA, USA). RNAiso Plus was purchased from Takara Bio (Kyoto, Japan). Rottlerin was purchased from Merk Millipore (Billerica, MA, USA). All other chemicals were of analytical grade.

Mizuguchi H., Wakugawa T., Sadakata H., Kamimura S., Takemoto M., Nakagawa T., Yabumoto M., Kitamura Y., Takeda N, & Fukui H. (2020). Elucidation of Inverse Agonist Activity of Bilastine. Pharmaceutics, 12(6), 525.

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Optimizing siRNA-NG and LNP Transfection

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H1299-eGFP cells were seeded at a cell density of 8000 cells/well in 96-well plates (Bioswisstec, Schaffhausen, Switzerland) and were allowed to settle overnight. The next day, siRNA-NG complexes were prepared as described above with siRNA concentrations ranging from 0.05-250 nM and diluted 5-fold in Opti-MEM before being applied on cells for 4 h. On the other hand, for transfections with LNPs, the carrier was diluted in CCM and applied on cells for 24 h. Next, transfection medium was removed and cells were washed with PBS -/-and incubated for 20 h with lofepramine 30 µM (Sanbio, Uden, Netherlands), desloratadine 30 µM (Sigma-Aldrich, Overijse, Belgium) and ebastine 15 µM (Sanbio, Uden, Netherlands). Following Lysotracker Deep Red (LDR) stain (Thermo Fisher Scientific, Waltham, MA, USA) in CCM for 30 min at 37°C. Expression of eGFP and LDR staining was detected via flow cytometry, using a CytoFLEX flow cytometer plate reader for 96-well plates (Beckman Coulter, Krefeld, Germany) and CytExpert software. Data analysis was performed using the FlowJo analysis software (Treestar, Costa Mesa, CA, USA) and the percentage of eGFP expression for each sample was calculated by normalizing the fluorescence signal of cells treated with siEGFP to the fluorescence of cells treated with siCTRL.

Muntean C., Blondeel E., Harinck L., Pednekar K., Prakash J., De Wever O., Chain J.L., De Smedt S.C., Remaut K, & Raemdonck K. (2023). Repositioning the antihistamine ebastine as an intracellular siRNA delivery enhancer. International journal of pharmaceutics, 644.

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Formulation and Characterization of Desloratadine Tablets

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Desloratadine (raw material) was gifted by Wimits Pharmaceuticals Pvt Ltd. Lactose, talc, magnesium stearate, mannitol were purchased from Sigma-Aldrich (Germany). Aspartame, PVP, IPA, Avicel 101 were purchased from Midland Scientific Inc.

Abbas M., Abbas M., Tariq F., Yasin R., & Nabeel M. (2020). Formulation and evaluation of chewable tablets of Desloratadine prepared by aqueous and non-aqueous techniques. Journal of Drug Delivery and Therapeutics, 10(1), 5-10.

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