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
References
Oct 26, 1978·The New England Journal of Medicine·S P GalantP A Insel
Jan 1, 1992·Trends in Pharmacological Sciences·P J Barnes, K F Chung
Oct 22, 1992·The New England Journal of Medicine·D CheungP J Sterk
Oct 22, 1992·The New England Journal of Medicine·B J O'ConnorP J Barnes
Feb 25, 1991·European Journal of Pharmacology·Q A HamidP J Barnes
Aug 1, 1990·Chest·R W HauckE Erdmann
Dec 8, 1990·Lancet·M R SearsG P Herbison
Apr 1, 1987·Analytical Biochemistry·P Chomczynski, N Sacchi
Oct 14, 1986·European Journal of Pharmacology·D J DooleyN C Reymann
Jul 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·J R Hadcock, C C Malbon
Sep 1, 1985·The Journal of Clinical Investigation·O E BroddeA Daul
Sep 1, 1987·The Journal of Allergy and Clinical Immunology·H MeursK de Vries
Oct 1, 1995·American Journal of Respiratory and Critical Care Medicine·D H YatesK F Chung
Jul 1, 1995·The Journal of Clinical Investigation·J C MakP J Barnes
Aug 24, 1995·The New England Journal of Medicine·H S Nelson
Sep 1, 1995·American Journal of Respiratory and Critical Care Medicine·P J Barnes
Jun 1, 1995·American Journal of Respiratory and Critical Care Medicine·N D ManolitsasR J Davies
Jan 1, 1995·The American Journal of Physiology·J C MakP J Barnes
Oct 2, 1993·Lancet·D W CockcroftB C Rutherford
Oct 15, 1993·European Journal of Pharmacology·M NishikawaP J Barnes
Jan 1, 1994·American Journal of Respiratory Cell and Molecular Biology·M NishikawaP J Barnes
Aug 1, 1993·Chest·I HataokaK Shirato
Feb 1, 1993·Thorax·D R TaylorQ Li
Citations
Jul 1, 2008·Expert Review of Clinical Immunology·Jeffrey B Rubins
Apr 16, 2004·Drugs & Aging·Shelley R Salpeter
Dec 4, 2004·Immunogenetics·Robert WestlandEddy A Wierenga
May 3, 2011·Biological & Pharmaceutical Bulletin·Qian ShiGang Bai
Aug 4, 2015·Expert Opinion on Drug Metabolism & Toxicology·Kathryn Blake, John Lima
Jul 23, 1998·Biology of Reproduction·J L LécrivainJ P Maltier
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
Feb 6, 2003·British Journal of Pharmacology·Lee K ChongPeter T Peachell
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