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Desoye, G; Ertl-Stockinger, U; Porta, S.
Prolonged administration in vivo of alpha and beta adrenergic agonists decreases insulin binding to rat myocardial membranes in vitro by different mechanisms.
LIFE SCI 1991 48: 2249-2258. Doi: 10.1016%2F0024-3205%2891%2990340-H
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Leading authors Med Uni Graz
Desoye Gernot
Co-authors Med Uni Graz
Porta Sepp
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Abstract:
Male Sprague Dawley rats were continuously treated in vivo for 6, 12 and 20 hours with a combination of an alpha- (beta-) adrenoreceptor agonist and a beta- (alpha-) adrenoreceptor antagonist in subcutaneously implanted depot tablets. Crude membranes prepared from myocardial cells exhibited a decreased maximum binding of [125I]-insulin after 20 hours irrespective of the treatment applied. Scatchard and non-linear regression analysis of the displacement curves assuming two non-cooperative binding sites revealed a downregulation of the high affinity receptors for about 85% and a concomitant 2.5-fold increased receptor affinity under beta-adrenergic influence. In contrast, alpha-adrenergic treatment did not affect the receptor number but decreased the high affinity by 70%. The low affinity binding sites were virtually unaffected by the different treatments. The phospholipid and cholesterol contents of the membranes were not significantly altered. The phospholipid/cholesterol ratios after 12 and 20 hours of alpha-adrenergic treatment, however, were decreased. We suggest that the decreased binding activity of insulin receptors on rat myocardial membranes after continuous in vivo treatment with alpha- and beta- adrenergic agonists is mediated by different mechanisms.
Find related publications in this database (using NLM MeSH Indexing)
Adrenergic alpha-Agonists - pharmacology
Adrenergic beta-Agonists - pharmacology
Animals - pharmacology
Blood Glucose - metabolism
Drug Administration Schedule - metabolism
Drug Implants - metabolism
Heart - drug effects
Kinetics - drug effects
Male - drug effects
Myocardium - metabolism
Rats - metabolism
Rats, Inbred Strains - metabolism
Receptor, Insulin - drug effects

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