These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Different effects of beta-adrenoceptor desensitization on inhibitory actions in guinea-pig trachealis.
    Author: Mizutani H, Kume H, Ito Y, Takagi K, Yamaki K.
    Journal: Clin Exp Pharmacol Physiol; 2002 Aug; 29(8):646-54. PubMed ID: 12099994.
    Abstract:
    1. To determine the inhibitory effects of agents that pass through and bypass beta-adrenoceptors under conditions of tolerance to beta-adrenoceptor agonists, we examined the inhibition by the beta-adrenoceptor agonists forskolin and theophylline against contraction induced by methacholine (MCh) after exposure to higher concentrations of a beta-adrenoceptor agonist for a long time in guinea-pig tracheal smooth muscle, using isometric tension records. 2. After exposure to procaterol (0.0003-3 micromol/L) for 45 min, the inhibitory effect of 0.03 micromol/L procaterol on 1 micromol/L MCh-induced contraction was attenuated in a concentration-dependent manner, whereas after exposure to isoprenaline (0.0003-3 micromol/L) for an equivalent time, the inhibitory effect of isoprenaline was markedly attenuated at each concentration. However, after exposure to 3 micromol/L procaterol for 45 min, the inhibitory actions of forskolin and theophylline were, conversely, augmented. 3. These phenomena were observed under conditions whereby the response to MCh returned to control levels 6 h after removal of 3 micromol/L procaterol. The percentage inhibition produced by 0.1 micromol/L forskolin against 1 micromol/L MCh after exposure to normal bathing solution or 3 micromol/L procaterol for 45 min was 9.8 +/- 5.5 and 82.8 +/- 6.5%, respectively (P < 0.001). These values for 100 micromol/L (18 microg/mL) theophylline on MCh resposnes were 9.9 +/- 8.5 and 88.0 +/- 4.4% (n = 6 for both), respectively (P < 0.001). 4. The inhibitory action of agents that bypass beta-adrenoceptors was markedly augmented under conditions of beta-adrenoceptor desensitization in airway smooth muscle. 5. In conclusion, procaterol is less potent in causing desensitization of beta-adrenoceptors than isoprenaline. The activity of adenylyl cyclase may be enhanced after exposure to a high concentration of beta-adrenoceptor agonists.
    [Abstract] [Full Text] [Related] [New Search]