Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes.
Article Details
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Yasuda SU, Yasuda RP
Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes.
Pharmacotherapy. 1999 Apr;19(4):447-51.
- PubMed ID
- 10212017 [ View in PubMed]
- Abstract
Anticholinergic effects are presumed to be the mechanism for the efficacy of chlorpheniramine in symptomatic relief of the common cold. Terfenadine, a second-generation antihistamine, reportedly lacks anticholinergic side effects. We evaluated affinities of two commonly used over-the-counter antihistamines, brompheniramine and chlorpheniramine, as well as terfenadine in comparison with atropine at the five human muscarinic cholinergic receptor subtypes using CHO cells stably transfected with the individual subtypes. Atropine was more potent than all three drugs at m1-m5 (p<0.01). No significant difference was observed between chlorpheniramine and brompheniramine. Atropine, brompheniramine, and chlorpheniramine could not discriminate between m1-m5. Terfenadine demonstrated subtype selectivity at m3. In vitro comparisons in human muscarinic receptor subtypes could potentially be used to predict clinical anticholinergic effects of antihistamines and to target receptor-specific effects of such agents.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Brompheniramine Histamine H1 receptor Protein Humans YesAntagonistDetails Brompheniramine Muscarinic acetylcholine receptor M1 Protein Humans UnknownAntagonistDetails Brompheniramine Muscarinic acetylcholine receptor M2 Protein Humans UnknownAntagonistDetails Brompheniramine Muscarinic acetylcholine receptor M3 Protein Humans UnknownAntagonistDetails Brompheniramine Muscarinic acetylcholine receptor M4 Protein Humans UnknownAntagonistDetails Brompheniramine Muscarinic acetylcholine receptor M5 Protein Humans UnknownAntagonistDetails Terfenadine Muscarinic acetylcholine receptor M1 Protein Humans UnknownBinderDetails Terfenadine Muscarinic acetylcholine receptor M2 Protein Humans UnknownBinderDetails Terfenadine Muscarinic acetylcholine receptor M3 Protein Humans UnknownAntagonistDetails Terfenadine Muscarinic acetylcholine receptor M4 Protein Humans UnknownBinderDetails Terfenadine Muscarinic acetylcholine receptor M5 Protein Humans UnknownBinderDetails