ArticleBritish journal of pharmacology2011
Formoterol and salmeterol induce a similar degree of β2-adrenoceptor tolerance in human small airways but via different mechanisms.
Article in British journal of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
25 citing papers in PubMed, 42 citations in OpenAlex.
- Functional respiratory imaging assessment of budesonide/glycopyrrolate/formoterol fumarate and glycopyrrolate/formoterol fumarate metered dose inhalers in patients with COPD: the value of inhaled corticosteroids.Respiratory research · 2021Trial
- Fixed airflow obstruction in asthma: a descriptive study of patient profiles and effect on treatment responses.The Journal of asthma : official journal of the Association for the Care of Asthma · 2014Trial
- TMEM16A Antagonism: Therapeutic Potential with Desensitization of β-Agonist Responsiveness in Asthma.American journal of respiratory cell and molecular biology · 2025Article
- Precision cut lung slices: an integrated ex vivo model for studying lung physiology, pharmacology, disease pathogenesis and drug discovery.Respiratory research · 2024Review
- Starving a Cell Promotes Airway Smooth Muscle Relaxation: Inhibition of Glycolysis Attenuates Excitation-Contraction Coupling.American journal of respiratory cell and molecular biology · 2023Article
- Perspectives on precision cut lung slices-powerful tools for investigation of mechanisms and therapeutic targets in lung diseases.Frontiers in pharmacology · 2023Review
- Epinephrine evokes shortening of human airway smooth muscle cells following βAmerican journal of physiology. Lung cellular and molecular physiology · 2022Article
- Airway smooth muscle function in asthma.Frontiers in physiology · 2022Review
- Organotypic Models of Lung Cancer.Current topics in microbiology and immunology · 2021Article
- G Protein-Coupled Receptors in Asthma Therapy: Pharmacology and Drug Action.Pharmacological reviews · 2020Review
- Acetaminophen is both bronchodilatory and bronchoprotective in human precision cut lung slice airways.Xenobiotica; the fate of foreign compounds in biological systems · 2019Article
- Effects of rhinovirus 39 infection on airway hyperresponsiveness to carbachol in human airways precision cut lung slices.The Journal of allergy and clinical immunology · 2018Article
- Review
- Airway Relaxation Effects of Water-Soluble Sclerotial Extract FromFrontiers in pharmacology · 2018Article
- Inhibition of PI3K promotes dilation of human small airways in a rho kinase-dependent manner.British journal of pharmacology · 2016Article
- Development of an Ex Vivo Tissue Platform To Study the Human Lung Response to Coxiella burnetii.Infection and immunity · 2016Article
- Soluble guanylate cyclase as an alternative target for bronchodilator therapy in asthma.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- Salmeterol Efficacy and Bias in the Activation and Kinase-Mediated Desensitization of β2-Adrenergic Receptors.Molecular pharmacology · 2015Article
- Functional desensitization of the β 2 adrenoceptor is not dependent on agonist efficacy.Pharmacology research & perspectives · 2015Article
- ASM-024, a piperazinium compound, promotes the in vitro relaxation of β2-adrenoreceptor desensitized tracheas.PloS one · 2015Article
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeSteroids prevent and reverse salbutamol-induced β(2)-adrenoceptor tolerance in human small airways. This study examines the effects of the long-acting β(2) agonists (LABAs) formoterol and salmeterol, and the ability of budesonide to prevent desensitization. EXPERIMENTAL APPROACH: Long-acting β(2) agonists in the presence and absence of budesonide were incubated with human precision-cut lung slices containing small airways. Tolerance was deduced from measurements of reduced bronchodilator responses to isoprenaline and correlated with β(2)-adrenoceptor trafficking using a virally transduced, fluorescent-tagged receptor. The ability of the LABAs to protect airways against muscarinic-induced contraction was also assessed. KEY
resultsFollowing a 12 h incubation, both formoterol and salmeterol attenuated isoprenaline-induced bronchodilatation to a similar degree and these effects were not reversible by washing. Pre-incubation with budesonide prevented the desensitization induced by formoterol, but not that induced by salmeterol. Formoterol also protected the airways from carbachol-induced bronchoconstriction to a greater extent than salmeterol. In the epithelial cells of small airways, incubation with formoterol promoted receptor internalization but this did not appear to occur following incubation with salmeterol. Budesonide inhibited the formoterol-induced reduction in plasma membrane β(2)-adrenoceptor fluorescence. CONCLUSIONS AND IMPLICATIONS: Although both formoterol and salmeterol attenuate isoprenaline-induced bronchodilatation, they appear to induce β(2)-adrenoceptor tolerance via different mechanisms; formoterol, but not salmeterol, enhances receptor internalization. Budesonide protection against β(2)-adrenoceptor tolerance was correlated with the retention of receptor fluorescence on the plasma membrane, thereby suggesting a mechanism by which steroids alter β(2)-adrenoceptor function.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.