ArticleAmerican journal of physiology. Lung cellular and molecular physiology2012
The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea.
Article in American journal of physiology. Lung cellular and molecular physiology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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42 citing papers in PubMed, 86 citations in OpenAlex.
- Evaluation of Bronchial Receptors with Concentration-Response Curves, Bitterness Assessment, and Computer Simulations.Cell biochemistry and biophysics · 2026Article
- Daytime-Dependent Effects of Thiamine on the Thiamine Pool and Pyruvate Dehydrogenase Regulation in the Brain and Heart.International journal of molecular sciences · 2025Article
- Spatiotemporal calcium signaling patterns underlying opposing effects of histamine and TAS2R agonists in airway smooth muscle.American journal of physiology. Lung cellular and molecular physiology · 2025Article
- Denatonium inhibits RANKL-induced osteoclast differentiation and rescues the osteoporotic phenotype by blocking p65 signaling pathway.Molecular medicine (Cambridge, Mass.) · 2024Article
- Bitter tastants relax the mouse gallbladder smooth muscle independent of signaling through tuft cells and bitter taste receptors.Scientific reports · 2024Article
- Molecular mechanism of bitter taste receptor agonist-mediated relaxation of airway smooth muscle.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2024Article
- Bitter Taste Receptor Agonist Denatonium Inhibits Stemness Characteristics in Hematopoietic Stem/Progenitor Cells.Stem cells (Dayton, Ohio) · 2024Article
- Review
- Bitter Taste Receptors in the Airway Cells Functions.Handbook of experimental pharmacology · 2022Article
- Acrid and Bitter Chinese Herbs in Decoction Effectively Relieve Lung Inflammation and Regulation of TRPV1/TAS2R14 Channels in a Rat Asthmatic Model.Evidence-based complementary and alternative medicine : eCAM · 2022Article
- Chloroquine Attenuates Asthma Development by Restoring Airway Smooth Muscle Cell PhenotypeFrontiers in pharmacology · 2022Article
- Diacylglycerol Kinase Inhibition Reduces Airway Contraction by Negative Feedback Regulation of Gq-Signaling.American journal of respiratory cell and molecular biology · 2021Article
- Review
- An update on extra-oral bitter taste receptors.Journal of translational medicine · 2021Review
- Genetic deletion of the Tas2r143/Tas2r135/Tas2r126 cluster reveals that TAS2Rs may not mediate bitter tastant-induced bronchodilation.Journal of cellular physiology · 2021Article
- Chloroquine: Autophagy inhibitor, antimalarial, bitter taste receptor agonist in fight against COVID-19, a reality check?European journal of pharmacology · 2021Review
- Treatment Protocol for COVID-19 Based on T2R Phenotype.Viruses · 2021Article
- Can GPCRs Be Targeted to Control Inflammation in Asthma?Advances in experimental medicine and biology · 2021Article
- Denatonium as a Bitter Taste Receptor Agonist Modifies Transcriptomic Profile and Functions of Acute Myeloid Leukemia Cells.Frontiers in oncology · 2020Article
- Effects of MP-AzeFlu enhanced by activation of bitter taste receptor TAS2R.Allergy, asthma, and clinical immunology : official journal of the Canadian Society of Allergy and Clinical Immunology · 2020Article
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Authors and funding
5 authors at 2 institutions in 2 countries.
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No grant is acknowledged in the PubMed record.
Abstract
Activation of taste receptors (TAS2Rs) by bitter taste agonists has been reported to cause bronchodilation. The aim of this study was to extend the information on the effects of bitter taste agonists on responses induced by different contractile mediators in a standard airway physiology preparation. Isometric responses were assessed in guinea pig trachea (GPT). TAS2R agonists were administered either to segments precontracted with different agonists for contraction or given before challenge with the different contractile stimuli, including antigen in tissues from ovalbumin-sensitized animals. TAS2R mRNA expression on GPT epithelium and smooth muscle was measured with real-time PCR. Denatonium, chloroquine, thiamine, and noscapine induced concentration-dependent relaxations (R(max): 98.3 ± 1.6, 100.0 ± 0.0, 100.0 ± 0.0, and 52.3 ± 1.1% of maximum, respectively, in the presence of indomethacin) in segments precontracted with carbachol. The receptors for denatonium (TAS2R4, TAS2R10) and chloroquine (TAS2R3, TAS2R10) were expressed in GPT. Whereas denatonium selectively inhibited contractions induced by carbachol, chloroquine uniformly inhibited contractions evoked by prostaglandin E(2), the thromboxane receptor agonist U-46619, leukotriene D(4), histamine, and antigen. The effects of denatonium, but not those of chloroquine, were partly inhibited by blockers of the large Ca(2+)-activated K(+) channels and decreased by an increase of the level of precontraction. In conclusion, TAS2R agonists mediated strong relaxations and substantial inhibition of contractions in GPT. Chloroquine and denatonium had distinct patterns of activity, indicating different signaling mechanisms. The findings reinforce the hypothesis that TAS2Rs are potential targets for the development of a new class of more efficacious agonists for bronchodilation.
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