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Exposure to (-)-isoprenaline (25 microM, 1 h) caused a stereoselective, time and concentration-related decrease in smooth muscle beta 2-adrenoceptor function in guinea-pig trachea. Furthermore, tracheal relaxant responsiveness to the beta-adrenoceptor agonists (+/-)-fenoterol and (-)-noradrenaline was reduced, while that to theophylline and nitroprusside was unaffected. Responsiveness to forskolin was marginally but significantly reduced. Indomethacin, a cyclooxygenase inhibitor and mepacrine, an inhibitor of phospholipid turnover, had no significant effect on the extent of isoprenaline-induced desensitization. Conversely, cortisol (25 microM) significantly reduced desensitization and enhanced the rate of spontaneous recovery of responsiveness to isoprenaline. Desensitization was not accompanied by a reduction in the density of beta-adrenoceptors in the trachea, as assessed by binding and light microscopic autoradiography using [125I]iodocyanopindolol [( 125I]CYP). Thus, desensitization was probably caused primarily by beta-adrenoceptor/adenyl cyclase uncoupling. This model may be useful in investigations of the effect of glucocorticoids on the beta-adrenoceptor dysfunction recognized in severe asthma.
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
July 1987,
Zhongguo yao li xue bao = Acta pharmacologica Sinica,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
March 1990,
European journal of pharmacology,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
January 1983,
Advances in prostaglandin, thromboxane, and leukotriene research,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
January 1997,
The Journal of pharmacology and experimental therapeutics,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
January 1989,
Pulmonary pharmacology,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
June 1981,
European journal of pharmacology,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
January 1995,
Acta physiologica et pharmacologica Bulgarica,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
January 1990,
Pharmacological research,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
December 1982,
Journal of autonomic pharmacology,
L B Fernandes, and
D A Knight, and
P J Rigby, and
D Spina, and
J W Paterson, and
R G Goldie
January 1989,
Fundamental & clinical pharmacology,
