Effects of chronic administration of agonists and antagonists on the density of beta-adrenergic receptors

Kim A. Neve, Perry B. Molinoff

Research output: Contribution to journalArticle

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Abstract

It is frequently hypothesized that drug-induced alterations in the density of β-adrenergic receptors underlie tolerance to and physical dependence on agonists and antagonists at β-adrenergic receptors. Two approaches to determining the effect of treatment with drugs on the density of β-adrenergic receptors are described. In the first, the density of β-adrenergic receptors was measured on leukocytes taken from human subjects during and after drug treatment. Treatment with the antagonist propranolol caused an increase in the density of β-adrenergic receptors on leukocytes, whereas treatment with the agonists terbutaline and ephedrine, or pindolol, an antagonist with intrinsic sympathomimetic activity, caused a decrease in the density of β-adrenergic receptors. In the second approach, the effect of agonists on the density of β-adrenergic receptors on C6 glioma cells in culture was determined. Incubation with the full agonist isoproterenol decreased the density of both β1 and β2-adrenergic receptors. In contrast, incubation with pindolol or celiprolol, also an antagonist with intrinsic sympathomimetic activity, selectively decreased the density of β2-adrenergic receptors. Pindolol and celiprolol may be useful in situations in which selective stimulation of β2-adrenergic receptors and blockade of β1-adrenergic receptors is desirable.

Original languageEnglish (US)
Pages (from-to)F17-F22
JournalThe American journal of cardiology
Volume57
Issue number12
DOIs
StatePublished - Apr 25 1986

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ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine

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