The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea.
Identifieur interne : 001297 ( Main/Exploration ); précédent : 001296; suivant : 001298The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea.
Auteurs : Ville Pulkkinen [Suède] ; Martijn L. Manson ; Jesper S Fholm ; Mikael Adner ; Sven-Erik DahlénSource :
- American journal of physiology. Lung cellular and molecular physiology [ 1522-1504 ] ; 2012.
Descripteurs français
- KwdFr :
- Agonistes cholinergiques (pharmacologie), Animaux, Bronchodilatateurs (pharmacologie), Canaux potassiques calcium-dépendants de grande conductance (antagonistes et inhibiteurs), Canaux potassiques calcium-dépendants de grande conductance (métabolisme), Canaux potassiques calcium-dépendants de grande conductance (physiologie), Carbachol (pharmacologie), Charybdotoxine (pharmacologie), Chloroquine (pharmacologie), Cochons d'Inde, Composés d'ammonium quaternaire (pharmacologie), Contraction musculaire (), Expression des gènes, Indoles (pharmacologie), Indométacine (pharmacologie), Muqueuse respiratoire (), Muscles lisses (), Muscles lisses (physiologie), Mâle, Peptides (pharmacologie), Relâchement musculaire (), Récepteurs couplés aux protéines G (agonistes), Récepteurs couplés aux protéines G (génétique), Récepteurs couplés aux protéines G (métabolisme), Salbutamol (pharmacologie), Techniques in vitro, Trachée (), Trachée (métabolisme), Trachée (physiologie).
- MESH :
- agonistes : Récepteurs couplés aux protéines G.
- antagonistes et inhibiteurs : Canaux potassiques calcium-dépendants de grande conductance.
- génétique : Récepteurs couplés aux protéines G.
- métabolisme : Canaux potassiques calcium-dépendants de grande conductance, Récepteurs couplés aux protéines G, Trachée.
- pharmacologie : Agonistes cholinergiques, Bronchodilatateurs, Carbachol, Charybdotoxine, Chloroquine, Composés d'ammonium quaternaire, Indoles, Indométacine, Peptides, Salbutamol.
- physiologie : Canaux potassiques calcium-dépendants de grande conductance, Muscles lisses, Trachée.
- Animaux, Cochons d'Inde, Contraction musculaire, Expression des gènes, Muqueuse respiratoire, Muscles lisses, Mâle, Relâchement musculaire, Techniques in vitro, Trachée.
English descriptors
- KwdEn :
- Albuterol (pharmacology), Animals, Bronchodilator Agents (pharmacology), Carbachol (pharmacology), Charybdotoxin (pharmacology), Chloroquine (pharmacology), Cholinergic Agonists (pharmacology), Gene Expression, Guinea Pigs, In Vitro Techniques, Indoles (pharmacology), Indomethacin (pharmacology), Large-Conductance Calcium-Activated Potassium Channels (antagonists & inhibitors), Large-Conductance Calcium-Activated Potassium Channels (metabolism), Large-Conductance Calcium-Activated Potassium Channels (physiology), Male, Muscle Contraction (drug effects), Muscle Relaxation (drug effects), Muscle, Smooth (drug effects), Muscle, Smooth (physiology), Peptides (pharmacology), Quaternary Ammonium Compounds (pharmacology), Receptors, G-Protein-Coupled (agonists), Receptors, G-Protein-Coupled (genetics), Receptors, G-Protein-Coupled (metabolism), Respiratory Mucosa (drug effects), Trachea (drug effects), Trachea (metabolism), Trachea (physiology).
- MESH :
- chemical , agonists : Receptors, G-Protein-Coupled.
- chemical , antagonists & inhibitors : Large-Conductance Calcium-Activated Potassium Channels.
- chemical , genetics : Receptors, G-Protein-Coupled.
- chemical , metabolism : Large-Conductance Calcium-Activated Potassium Channels, Receptors, G-Protein-Coupled.
- chemical , pharmacology : Albuterol, Bronchodilator Agents, Carbachol, Charybdotoxin, Chloroquine, Cholinergic Agonists, Indoles, Indomethacin, Peptides, Quaternary Ammonium Compounds.
- chemical , physiology : Large-Conductance Calcium-Activated Potassium Channels.
- drug effects : Muscle Contraction, Muscle Relaxation, Muscle, Smooth, Respiratory Mucosa, Trachea.
- metabolism : Trachea.
- physiology : Muscle, Smooth, Trachea.
- Animals, Gene Expression, Guinea Pigs, In Vitro Techniques, Male.
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.
DOI: 10.1152/ajplung.00205.2012
PubMed: 22962016
Affiliations:
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qualifier="pharmacologie" xml:lang="fr"><term>Agonistes cholinergiques</term><term>Bronchodilatateurs</term><term>Carbachol</term><term>Charybdotoxine</term><term>Chloroquine</term><term>Composés d'ammonium quaternaire</term><term>Indoles</term><term>Indométacine</term><term>Peptides</term><term>Salbutamol</term></keywords><keywords scheme="MESH" qualifier="physiologie" xml:lang="fr"><term>Canaux potassiques calcium-dépendants de grande conductance</term><term>Muscles lisses</term><term>Trachée</term></keywords><keywords scheme="MESH" qualifier="physiology" xml:lang="en"><term>Muscle, Smooth</term><term>Trachea</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Gene Expression</term><term>Guinea Pigs</term><term>In Vitro Techniques</term><term>Male</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Cochons d'Inde</term><term>Contraction musculaire</term><term>Expression des gènes</term><term>Muqueuse respiratoire</term><term>Muscles lisses</term><term>Mâle</term><term>Relâchement musculaire</term><term>Techniques in vitro</term><term>Trachée</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">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.</div></front></TEI><affiliations><list><country><li>Suède</li></country><region><li>Svealand</li></region><settlement><li>Stockholm</li></settlement></list><tree><noCountry><name sortKey="Adner, Mikael" sort="Adner, Mikael" uniqKey="Adner M" first="Mikael" last="Adner">Mikael Adner</name><name sortKey="Dahlen, Sven Erik" sort="Dahlen, Sven Erik" uniqKey="Dahlen S" first="Sven-Erik" last="Dahlén">Sven-Erik Dahlén</name><name sortKey="Manson, Martijn L" sort="Manson, Martijn L" uniqKey="Manson M" first="Martijn L" last="Manson">Martijn L. Manson</name><name sortKey="S Fholm, Jesper" sort="S Fholm, Jesper" uniqKey="S Fholm J" first="Jesper" last="S Fholm">Jesper S Fholm</name></noCountry><country name="Suède"><region name="Svealand"><name sortKey="Pulkkinen, Ville" sort="Pulkkinen, Ville" uniqKey="Pulkkinen V" first="Ville" last="Pulkkinen">Ville Pulkkinen</name></region></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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