Azelastine hydrochloride

Manufactured by Merck Group

Sourced in United States

Azelastine hydrochloride is a pharmaceutical compound used as an active ingredient in various medications. It functions as an antihistamine, working to block the effects of the chemical histamine in the body. This compound is commonly utilized in the formulation of medications, particularly those intended for the treatment of allergic reactions and related conditions.

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Azelastine (3 citations) Hydrochlorides (2 citations)

8 protocols using azelastine hydrochloride

Azelastine Effects on HeLa Cells

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Human cervical adenocarcinoma cells (HeLa cells) were cultured in a Direct Heat incubator (Thermo Scientific, Waltham, MA, USA), under standard culture conditions, i.e., 37 °C and 5% CO₂, on a modified DMEM medium (GIBCO, New York, NY, USA), containing 10% fetal calf serum (Biowest, Nuaillé, France) and a mixture of antibiotics (penicillin G, streptomycin, amphotericin B) (Corning, Manassas, VA, USA). The HeLa cells were purchased from the American Type Tissue Culture Collection (Rockville, MD, USA). Cells were treated for 48 h with azelastine hydrochloride (≥98% HPLC), (4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl) phthalazin-1-one hydrochloride), which was purchased from Sigma Aldrich (St. Louis, MO, USA). The following concentrations of the test compound were used in the experiment: 15 µM, 25 µM, 45 µM, 60 µM, and 90 µM.
According to the literature data, the tested concentrations are used in research on antihistamine drugs conducted on cancer cell lines. Control cells were cultured in complete maintenance medium without the addition of the test compound.

Trybus E., Król T, & Trybus W. (2022). The Multidirectional Effect of Azelastine Hydrochloride on Cervical Cancer Cells. International Journal of Molecular Sciences, 23(11), 5890.

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Pharmaceutical Grade Standards Characterization

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Pharmaceutical grade standards of diphenhydramine hydrochloride (DIPH), azelastine hydrochloride (AZE) and bepotastine besylate (BEPO), papaverine and xylomethazoline hydrochlorides (the internal standards for HPLC methods) from Sigma-Aldrich (St. Louis, MO, USA), acetonitrile, methanol and water for chromatography from Merck (Darmstad, Germany), glacial acetic acid, sodium acetate, hydrochloric acid, sodium chloride, sodium tetraborate, phosphoric acid, sodium hydrogen phosphate, sodium dihydrogen phosphate, kalium dihydrogen phosphate and kalium hydroxide from POCh (Gliwice, Poland) were used. The buffer solutions, i.e., acetate buffer of pH 4, phosphate buffer of 7 and borate buffer of pH 10, were used as degradation media. Phosphate buffer of pH 3 was used for preparing the mobile phases in our HPLC methods. All buffers were prepared according to European Pharmacopoeia [18 ].

Gumieniczek A., Lejwoda K, & Data N. (2022). Chemical Stability Study of H1 Antihistaminic Drugs from the First and the Second Generations, Diphenhydramine, Azelastine and Bepotastine, in Pure APIs and in the Presence of Two Excipients, Citric Acid and Polyvinyl Alcohol. Molecules, 27(23), 8322.

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Cell Cycle Regulator Expression

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ADA, oxaliplatin, nilotinib, LS-194959, estradiol benzoate, nandrolone phenylpropionate, vilazodone, azelastine hydrochloride, latuda and paliperidone were purchased from Sigma-Aldrich. Anti-cyclin D, -B1 and -E as well as anti-CDK2, -Rb, phosphorylated (pho)-CDK2 (Thr-160), pho-Rb (Ser-795) and GAPDH were obtained from Cell Signaling Technology, Inc. (Danvers, MA, USA).

SHI X.N., LI H., YAO H., LIU X., LI L., LEUNG K.S., KUNG H.F, & LIN M.C. (2015). Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Molecular Medicine Reports, 12(5), 6501-6508.

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Antibiotic Dilution in M9 Medium

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Mepyramine maleate was obtained from Tocris Bioscience (Bristol, UK) and Sigma-Aldrich (St. Louis, MO, USA). Cetirizine dihydrochloride, azelastine hydrochloride, diphenhydramine hydrochloride, amoxicillin, sulfadiazine sodium salt, trimethoprim, enrofloxacin, colistin sulfate salt, gentamicin sulfate and kanamycin sulfate were purchased from Sigma-Aldrich (St. Louis, MO, USA). Tetracycline hydrochloride was obtained from Carl Roth (Karlsruhe, Germany) and florfenicol from Cayman Chemical Company (Ann Arbor, MI, USA). All agents were directly diluted in M9 minimal medium (described below), except florfenicol, which was first dissolved in 10 μl dimethyl sulfoxide (DMSO), and enrofloxacin by adding 5% of 1 N sodium hydroxide solution. The trimethoprim-potentiated sulfonamides were used at a ratio of 19:1 (sulfadiazine:trimethoprim) stock solution dissolved with 0.5 ml of DMSO in 20 ml M9 minimal medium.

Bruer G.G., Hagedorn P., Kietzmann M., Tohamy A.F., Filor V., Schultz E., Mielke-Kuschow S, & Meissner J. (2019). Histamine H1 receptor antagonists enhance the efficacy of antibacterials against Escherichia coli. BMC Veterinary Research, 15, 55.

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Biomolecular Interaction Analysis Protocol

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N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (EDC), N-hydroxysuccinimide (NHS), ethanolamine (EA) hydrochloride, K₂HPO₄, KH₂PO₄, NaCl, ethylenediaminetetraacetic acid (EDTA), NaOH, dimethyl sulfoxide (DMSO) and isopropyl β-d-1-thiogalactopyranoside (IPTG) were all obtained from Sigma-Aldrich (St. Louis, MO). Azelastine hydrochloride and bepridil were obtained from Sigma-Aldrich. Nutlin-3a was acquired from EMD Millipore Crop (Billerica, MA). Other reagents were of analytical purity and used as received. Solutions were prepared daily with deionized water from a Millipore system (Simplicity 185, Millipore Corp, Billerica, MA). Nitrilotriacetic acid (NTA) sensor chips were purchased from Biosensing Instrument Inc. (Tempe, AZ). Azelastine, bepridil, and nutlin-3a were separately dissolved in DMSO to afford 10 mM stock solutions, which were further diluted to 10 μM with the running buffer (10 mM sodium phosphate buffer containing 150 mM NaCl and 20 μM EDTA). Each drug candidate was mixed with 400 nM MDM2 and allowed to stand for 20 min at ambient temperature before SPR experiments. The final DMSO concentration in MDM2 and MDM2/drug mixtures was 0.1% (v/v).

Wang X., Magdziarz P., Enriquez E., Zhao W., Quan C., Darabedian N., Momand J, & Zhou F. (2019). Surface plasmon resonance and cytotoxicity assays of drug efficacies predicted computationally to inhibit p53/MDM2 interaction. Analytical biochemistry, 569, 53-58.

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Evaluating Azelastine's Antiviral Efficacy Against SARS-CoV-2 Variants

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Vero cells stably overexpressing human serine protease TMPRSS2 and ACE2 receptor (Riepler et al., 2021 (link)) were seeded on 96-well plates at 10⁴ cells/well the day before infection. Azelastine hydrochloride, (Sigma-Aldrich) was diluted with Dulbeccos`s Modified Eagle Medium (Merck, Darmstadt, Germany) containing 2% FBS to final concentrations ranging from 25 µM to 0.4 µM. Prior to infection of the cells, cell culture supernatant was aspirated and replaced with 50 µl of the Azelastine-HCl dilutions in the preventive (co-administration) setting and 50 µl of medium in the post-infection (therapeutic) setting. Subsequently, cells were infected with 50 µl of SARS-CoV-2 isolates carrying either the spike protein substitution D614G or belonging to the B.1.1.7 (alpha), B.1.351 (beta) or B.1.617.2 (delta) variants at an MOI of 0.01 for 30 min at 37°C. For both experimental settings, the supernatant then was aspirated and replaced by 50 µl fresh medium and 50 µl of the same azelastine concentrations used before, resulting in Azelastine concentrations ranging between 12.5 and 0.2 µM. 48 h post infection, the cytopathic effect was evaluated and supernatant was used to determine RNA copy number by quantitative real-time PCR.
Experiments with SARS-CoV-2 variants were performed at the Institute of Virology at the Medical University of Innsbruck according to institutional regulations.

Konrat R., Papp H., Kimpel J., Rössler A., Szijártó V., Nagy G., Madai M., Zeghbib S., Kuczmog A., Lanszki Z., Gesell T., Helyes Z., Kemenesi G., Jakab F, & Nagy E. (2022). The Anti-Histamine Azelastine, Identified by Computational Drug Repurposing, Inhibits Infection by Major Variants of SARS-CoV-2 in Cell Cultures and Reconstituted Human Nasal Tissue. Frontiers in Pharmacology, 13, 861295.

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Detailed Chemical Compound Acquisition Protocol

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The following chemicals were obtained from Sigma Aldrich Co. Ltd (Dorset, UK): azelastine hydrochloride (4-((4-chlorophenyl)methyl)-2-(1-methylazepan-4-yl)phthalazin-1-one hydrochloride; A7611), chlorhexidine digluconate (1,1′-hexamethylenebis(5-(p-chlorophenyl) biguanide; C9394), caffeine anhydrous (1,3,7-trimethylxanthine; W222402), quinine hydrochloride dihydrate (Q1125), acetaminophen (paracetamol, 4′-hydroxyacetanilide; A7085), ibuprofen sodium salt (α-methyl-4-(isobutyl) phenyl acetic acid; I1892), potassium nitrate (KNO 3 ; P8394), adenosine 3′,5′-cyclic monophosphate (3′,5′-cyclic AMP; A9501 -200mM stock solution), glucose (D(+)-glucose; G8270), sucrose (D(+)-saccharose; S1888) and glutamate (L-glutamic acid monosodium salt monohydrate; 49621). Compounds labelled "GSK" were provided by our industrial collaborators, Glaxo-SmithKline, and due to intellectual property protection, full names and structures have been withheld.

Cocorocchio M., Ives R., Clapham D., Andrews P.L, & Williams R.S. (2016). Bitter tastant responses in the amoeba Dictyostelium correlate with rat and human taste assays. ALTEX, 33(3).

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Evaluating Inhibitors of IL-31-Induced Pruritus

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Recombinant mouse IL-31 was prepared in Chugai Pharmaceutical Co., Ltd (Shizuoka, Japan). Briefly, IL-31 was purified from the supernatant of mouse IL-31-transformed Chinese hamster ovary cells using hydroxyapatite column (Bio-Rad Laboratories, Inc., Hercules, CA, USA), anion-exchange column (GE healthcare, Chicago, IL, USA), and gel filtration column (GE healthcare). IL-31 was dis-solved in phosphate buffered-saline (PBS) and administered intradermally. Naltrexone hydrochloride (Sigma-Aldrich, St Louis, MO, USA) (18) (19) (20) was dissolved in physiological saline and administered subcutaneously 15 min before IL-31 injection. Terfenadine (16, 18, 20) and tranilast (Sigma-Aldrich) (21) were dissolved in 0.5% sodium carboxymethyl cellulose and administered orally 30 and 60 min before IL-31 injection, respectively. Azelastine hydrochloride (Sigma-Aldrich) (16, 18, 22) was dissolved in tap water and administered orally 30 min before IL-31 injection. Indomethacin (Sigma-Aldrich) (15, 18) , zileuton (Ono Pharmaceutical Co. Ltd, Osaka, Japan) (15, 18, 23) , and CMHVA (5-[2-(2-carboxyethyl)-3-[6-(4-methoxyphenyl)-5E-hexenyl]oxyphenoxy] valeric acid) (Ono Pharmaceutical Co. Ltd) (15, 16, 18, 24, 25) ) were dissolved in 0.5% sodium carboxymethyl cellulose and administered orally 30, 60, and 60 min before IL-31 injection, respectively.

Andoh T., Harada A, & Kuraishi Y. (2017). Involvement of Leukotriene B4 Released from Keratinocytes in Itch-associated Response to Intradermal Interleukin-31 in Mice. Acta dermato-venereologica, 97(8).

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