Effect of short- and long-acting beta 2-adrenoceptor agonists on pulmonary beta 2-adrenoceptor expression in human lung

European Journal of Pharmacology
M NishikawaP J Barnes

Abstract

beta-Adrenoceptor agonists induce the down-regulation of beta 2-adrenoceptors and mRNA expression in animal lung. The down-regulation of beta 2-adrenoceptors may limit the therapeutic efficacy of beta 2-adrenoceptor-mediated bronchodilators in obstructive airways disease. We examined the effects of three selective beta 2-adrenoceptor agonists, salbutamol, salmeterol and formoterol on beta 2-adrenoceptor binding and mRNA levels in human lung in vitro. Human lung was obtained from cardiac transplantation donors. Peripheral lung was chopped and incubated with three selective beta 2-adrenoceptor agonist for 3 h or 24 h at three different concentrations (0.1, 1 and 10 microM). The affinity and density of beta 2-adrenoceptors was determined by [125I]iodocyanopindolol equilibrium binding in a lung membrane preparation in the presence of 0.1 microM CGP 20712 A (1-{2-[(3-carbamoyl-4-hydroxy)phenoxy] ethylamino}-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl) phenoxy]-propan-2-ol), a selective beta 1-adrenoceptor antagonist. Although treatment with salbutamol for 3 h did not change beta 2-adrenoceptor density, both salmeterol and formoterol reduced beta 2-adrenoceptor density, and exposure to each agonist for 24 h reduced beta 2-adrenocep...Continue Reading

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Citations

Jul 1, 2008·Expert Review of Clinical Immunology·Jeffrey B Rubins
Aug 4, 2015·Expert Opinion on Drug Metabolism & Toxicology·Kathryn Blake, John Lima
Aug 9, 2001·Annals of Medicine·D H AuB M Psaty
Mar 9, 2004·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·Catherine M Jackson, Brian Lipworth
May 28, 2011·American Journal of Respiratory Cell and Molecular Biology·Phillip FactorRachel L Miller
Feb 7, 2014·Allergy, Asthma, and Clinical Immunology : Official Journal of the Canadian Society of Allergy and Clinical Immunology·Ana Carolina Zimiani de PaivaCarmen Sílvia Bertuzzo
Mar 11, 2000·American Journal of Respiratory and Critical Care Medicine·D H AuB M Psaty
Oct 6, 2001·American Journal of Respiratory and Critical Care Medicine·J C Kips, R A Pauwels
Dec 24, 2005·Critical Care Medicine·Julien PottecherJacques Duranteau
Sep 19, 2002·British Journal of Clinical Pharmacology·Brian J Lipworth
Feb 28, 2002·European Journal of Pharmacology·Lee K ChongPeter T Peachell
Nov 6, 2009·Pulmonary Pharmacology & Therapeutics·Linda J KayPeter T Peachell

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