Anticholinergic properties of brompheniramine, chlorpheniramine, and atropine in human nasal mucosa in vitro. 1998

S Y Fang, and H M Druce, and J N Baraniuk
Division of Rheumatology, Immunology, and Allergy, Georgetown University, Washington, D.C. 20007-2197, USA.

Brompheniramine and chlorpheniramine have anticholinergic activities, but the relative potency of these effects has not been well defined. The anticholinergic properties of brompheniramine, chlorpheniramine, and atropine were assessed in an in vitro model of human nasal mucosal glandular secretion. Methacholine was used as a cholinergic agonist to stimulate glandular secretion of 7F10-mucin. These drugs (0.01-1000 microM) or vehicle (saline) were added to explant cultures with and without 100 microM methacholine. 7F10-mucin concentrations were measured in culture supernatants after 2-hour incubations. The effective dose reducing methacholine-induced secretion (ED50) was determined. ED50 was 0.25 microM for atropine, 4.10 microM for brompheniramine, and 4.63 microM for chlorpheniramine. None of the anticholinergic drugs changed spontaneous glandular exocytosis. Brompheniramine and chlorpheniramine are equipotent anticholinergic agents in human nasal mucosa in vitro. Atropine was 16 to 19 times more potent.

UI MeSH Term Description Entries
D009297 Nasal Mucosa The mucous lining of the NASAL CAVITY, including lining of the nostril (vestibule) and the OLFACTORY MUCOSA. Nasal mucosa consists of ciliated cells, GOBLET CELLS, brush cells, small granule cells, basal cells (STEM CELLS) and glands containing both mucous and serous cells. Nasal Epithelium,Schneiderian Membrane,Epithelium, Nasal,Membrane, Schneiderian,Mucosa, Nasal
D001977 Brompheniramine Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria. p-Bromdylamine,para-Bromdylamine,Brompheniramine Maleate,Brompheniramine Maleate (1:1),Chlorphed,Dimetane,Dimetane-Ten,Dimetapp Allergy,Oraminic-2,Dimetane Ten,Maleate, Brompheniramine,Oraminic 2,p Bromdylamine,para Bromdylamine
D002744 Chlorpheniramine A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE. Chlorphenamine,Chlorprophenpyridamine,Aller-Chlor,Antihistaminico Llorens,Chlo-Amine,Chlor-100,Chlor-Trimeton,Chlor-Tripolon,Chlorpheniramine Maleate,Chlorpheniramine Tannate,Chlorpro,Chlorspan 12,Chlortab-4,Cloro-Trimeton,Efidac 24,Kloromin,Piriton,Teldrin,Maleate, Chlorpheniramine,Tannate, Chlorpheniramine
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005089 Exocytosis Cellular release of material within membrane-limited vesicles by fusion of the vesicles with the CELL MEMBRANE.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001285 Atropine An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine. AtroPen,Atropin Augenöl,Atropine Sulfate,Atropine Sulfate Anhydrous,Atropinol,Anhydrous, Atropine Sulfate,Augenöl, Atropin,Sulfate Anhydrous, Atropine,Sulfate, Atropine
D016210 Methacholine Chloride A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116) Methacholine,2-(Acetyloxy)-N,N,N-trimethyl-1-propanaminium Chloride,Acetyl-2-methylcholine Chloride,Acetyl-beta-methacholine Chloride,Acetyl-beta-methylcholine,Mecholine,Mecholyl,Provocholine,Provokit,Acetyl 2 methylcholine Chloride,Acetyl beta methacholine Chloride,Acetyl beta methylcholine,Chloride, Methacholine
D046508 Culture Techniques Methods of maintaining or growing biological materials in controlled laboratory conditions. These include the cultures of CELLS; TISSUES; organs; or embryo in vitro. Both animal and plant tissues may be cultured by a variety of methods. Cultures may derive from normal or abnormal tissues, and consist of a single cell type or mixed cell types. Culture Technique,Technique, Culture,Techniques, Culture
D018680 Cholinergic Antagonists Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists. Acetylcholine Antagonist,Acetylcholine Antagonists,Anti-Cholinergic,Anticholinergic,Anticholinergic Agent,Anticholinergic Agents,Cholinergic Receptor Antagonist,Cholinergic-Blocking Agent,Cholinergic-Blocking Agents,Cholinolytic,Cholinolytics,Anti-Cholinergics,Anticholinergics,Cholinergic Antagonist,Cholinergic Receptor Antagonists,Agent, Anticholinergic,Agent, Cholinergic-Blocking,Agents, Anticholinergic,Agents, Cholinergic-Blocking,Antagonist, Acetylcholine,Antagonist, Cholinergic,Antagonist, Cholinergic Receptor,Antagonists, Acetylcholine,Antagonists, Cholinergic,Antagonists, Cholinergic Receptor,Anti Cholinergic,Anti Cholinergics,Cholinergic Blocking Agent,Cholinergic Blocking Agents,Receptor Antagonist, Cholinergic,Receptor Antagonists, Cholinergic

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