PMID: 8594305Jan 1, 1996Paper

Desensitization effect of in vivo treatment with metaproterenol on beta1, beta2 and beta3-adrenergic responsiveness in rat adipocytes

Life Sciences
M P PortilloJ A Martinez

Abstract

The desensitization process of beta-adrenergic system was assessed by in vivo administration to 7-week old rats of a mixed beta-agonist, metaproterenol (3,5-dehydroxyphenyl-N-isopropyl-amine-beta-ethanol sulphate; T1/2=6 hours), (2 mg/kg/d) in treatments of 12 hours, 2 days and 10 days. The in vitro lipolytic effect of selective beta-adrenergic agonists, dobutamine, salbutamol and BRL 37344, as well as plasma free fatty acid concentrations were measured in treated and control animals given vehicle. Different times of exposure to a beta-agonist induced a loss of responsiveness on lipolytic response mediated by beta1 and beta2-adrenoceptors, as demonstrated by decreased affinity and intrinsic activity (maximal effect) of dobutamine and salbutamol. In contrast, no changes were found in beta3 mediated lipolysis. These observations suggest that beta1, beta2 and beta3-adrenoceptors follow different regulatory patterns. Lack of beta3-adrenoceptor desensitization may have important physiological and therapeutic consequences in the treatment of diseases such as obesity and heart failure.

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Citations

Apr 2, 2003·Regulatory Peptides·Debbie L HayDavid M Smith
Oct 14, 2005·Obesity Research·Mary Anne Della-FeraClifton A Baile
Oct 26, 2018·American Journal of Respiratory Cell and Molecular Biology·Oleg S MatusovskyAnne-Marie Lauzon
Mar 6, 2010·American Journal of Respiratory Cell and Molecular Biology·Florian BossardChantal Gauthier
Dec 6, 2003·Eating and Weight Disorders : EWD·B BerraondoJ A Martinez
Dec 22, 2000·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·F Marion-LatardV Stich
Nov 27, 2020·BMC Pharmacology & Toxicology·Günther KrumplJuri Hodisch

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