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β_2-adrenoceptor in obstructive airway diseases:Agonism, antagonism or both?

World Journal of Respirology 2015年第3期5卷 199-206页

作者： Daniel WS Tan Jyi Lin Wong Siew Teck Tie john a abisheganaden Albert YH Lim WS Fred Wong Department of Pharmacology Yong Loo Lin School of MedicineNational University Health System Respiratory Unit Department of MedicineSarawak General Hospital Department of Respiratory and Critical Care Medicine Tan Tock Seng Hospital Immunology Program Life Science InstituteNational University of Singapore

Obstructive airway disease is a complex disease entity including several maladies characterized by bronchoconstriction and abnormal airway inflammation. Reversing bronchoconstriction leads to symptomatic relief and improvement in quality of life, both in reversible(bronchial asthma) and partially reversible(chronic obstructive airway disease) obstructive airway diseases. β2-adrenoceptor expressed in human airway is the main β-receptor subtype, and its activation in airway smooth muscle cells leads to bronchodilatation. Drugs targeting β-adrenoceptors have been around for many years, for which agonists of the receptors are used in bronchodilation while antagonists are used in cardiovascular diseases. This review article summarizes the effect and usage of β2-agonist in obstructive airway disease, addressing the benefits and potential risks of β2-agonist. The article also looks at the safety of β-blocker usage for cardiovascular disease in patients with obstructive airway disease. There is also emerging evidence that non-selective β-blockers with inverse agonism ironically can have longterm beneficial effects in obstructive airway disease that is beyond cardiovascular protection. Further trials are urgently needed in this area as it might lead to a dramatic turnaround in clinical practice for obstructive airway diseases as has already been seen in the usage of β-blockers for heart failure.

关键词： β-adrenoceptors β2-agonist β-blocker Inverse agonist Heart failure β-arrestin

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